U.S. patent application number 15/219852 was filed with the patent office on 2017-02-02 for topical skin formulations.
The applicant listed for this patent is MARY KAY INC.. Invention is credited to Edward Chadwick, Tiffany Florence, Geetha Kalahasti, Daniel Ramirez, Milagros Sanchez.
Application Number | 20170027843 15/219852 |
Document ID | / |
Family ID | 57885342 |
Filed Date | 2017-02-02 |
United States Patent
Application |
20170027843 |
Kind Code |
A1 |
Florence; Tiffany ; et
al. |
February 2, 2017 |
TOPICAL SKIN FORMULATIONS
Abstract
The present invention relates generally to methods and
compositions useful for application to skin and hair comprising
saccharide isomerate, hydrolyzed algin, zinc sulfate, and a
dermatologically acceptable vehicle, wherein the composition is
capable of moisturizing and/or improving the appearance and/or
condition of skin and/or hair.
Inventors: |
Florence; Tiffany; (Addison,
TX) ; Chadwick; Edward; (Addison, TX) ;
Sanchez; Milagros; (Addison, TX) ; Ramirez;
Daniel; (Addison, TX) ; Kalahasti; Geetha;
(Addison, TX) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
MARY KAY INC. |
Addison |
TX |
US |
|
|
Family ID: |
57885342 |
Appl. No.: |
15/219852 |
Filed: |
July 26, 2016 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
62197838 |
Jul 28, 2015 |
|
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|
Current U.S.
Class: |
1/1 |
Current CPC
Class: |
A61K 8/99 20130101; A61K
8/733 20130101; A61Q 19/10 20130101; A61K 8/9711 20170801; A61K
2800/782 20130101; A61Q 19/007 20130101; A61Q 1/12 20130101; A61K
8/0212 20130101; A61K 8/27 20130101; A61K 8/60 20130101; A61Q 19/00
20130101; A61K 2800/596 20130101; A61Q 19/008 20130101; A61Q 1/02
20130101; A61K 2800/78 20130101 |
International
Class: |
A61K 8/73 20060101
A61K008/73; A61K 8/27 20060101 A61K008/27; A61Q 19/10 20060101
A61Q019/10; A61K 8/60 20060101 A61K008/60; A61Q 19/00 20060101
A61Q019/00; A61Q 1/12 20060101 A61Q001/12 |
Claims
1. A method of treating a subject in need thereof comprising
applying a topical composition comprising saccharide isomerate,
hydrolyzed algin, zinc sulfate, and a dermatologically acceptable
vehicle to skin, wherein at least one of filaggrin production is
increased, skin moisture is increased, occludin production is
increased, TNF.alpha. production is inhibited, oxidative damage is
prevented, PPAR-.gamma. activity is inhibited, MMP1 is inhibited,
MMP9 is inhibited, or elastase is inhibited, wherein the saccharide
isomerate comprises an exopolysaccharide synthesized by Vibrio
alginolyticus, and wherein the hydrolyzed algin extract comprises
an anionic polysaccharide synthesized by Laminaria digitate.
2. The method of claim 1, wherein at least one of filaggrin
production is increased, skin moisture is increased, occludin
production is increased, TNF.alpha. production is inhibited, or
oxidative damage is prevented, and wherein at least one of
PPAR-.gamma. activity is inhibited, MMP1 is inhibited, MMP9 is
inhibited, or elastase is inhibited.
3. The method of claim 1, wherein the saccharide isomerate
increases production of filaggrin, increases skin moisture,
increases production of occluding, inhibits TNF.alpha. production,
and/or prevents oxidative damage, and/or the hydrolyzed algin and
zinc sulfate inhibit PPAR-.gamma. activity, inhibit MMP1 activity,
inhibit MMP9 activity, and/or inhibit elastase activity.
4. The method of claim 1, wherein the composition comprises 0.0001%
to 2% w/w of saccharide isomerate, 0.001% to 2% w/w of hydrolyzed
algin, and 0.0001% to 1% w/w of zinc sulfate.
5. The method of claim 1, wherein the composition is formulated as
at least one of a moisturizer, a mask, a foundation, a freshener,
and/or a cleanser.
6. The method of claim 1, wherein the wherein the dermatologically
acceptable vehicle comprises water.
7. The method of claim 6, wherein the composition comprises 30% to
98% w/w of water.
8. The method of claim 1, wherein skin of the subject is treated
and wherein the skin has an oily skin type.
9. A topical composition comprising saccharide isomerate,
hydrolyzed algin, zinc sulfate, and a dermatologically acceptable
vehicle, wherein the composition is capable of moisturizing at
least one of skin and/or hair, wherein the saccharide isomerate
comprises an exopolysaccharide synthesized by Vibrio alginolyticus,
and wherein the hydrolyzed algin extract comprises an anionic
polysaccharide synthesized by Laminaria digitate.
10. The composition of claim 9, wherein the composition comprises
an effective amount of saccharide isomerate capable of increasing
production of filaggrin, increasing skin moisture, increasing
production of occluding, inhibiting TNF.alpha. production, and/or
preventing oxidative damage, and/or wherein the composition
comprises an effective amount of hydrolyzed algin and zinc sulfate
capable of inhibiting PPAR-.gamma. activity, inhibiting MMP1
activity, inhibiting MMP9 activity, and/or inhibiting elastase
activity.
11. The composition of claim 9, wherein the composition comprises
0.0001% to 2% w/w of saccharide isomerate, 0.001% to 2% w/w of
hydrolyzed algin, and 0.0001% to 1% w/w of zinc sulfate.
12. The composition of claim 9, wherein the dermatologically
acceptable vehicle comprises water.
13. The composition of claim 12, wherein the composition comprises
30% to 98% w/w of water.
14. The composition of claim 9, wherein the composition is
formulated as at least one of a moisturizer, a mask, a foundation,
a freshener, and/or a cleanser.
15. The composition of claim 9, wherein the composition is
formulated to treat a subject's skin, wherein the skin has an oily
skin type.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of U.S. Provisional
Application No. 62/197,838 filed Jul. 28, 2015, the content of
which is incorporated into the present application by
reference.
BACKGROUND OF THE INVENTION
[0002] A. Field of the Invention
[0003] The present invention relates generally to the field of
cosmetics. More particularly, it concerns compositions that can be
used to moisturize, exfoliate, or prepare skin for moisturization.
In another aspect, the composition can be used as a cleanser or
freshener to remove residue, dirt, oil, grease, tars, etc., from
surfaces. In yet another aspect, the composition can be used as a
cosmetic foundation.
[0004] B. Description of Related Art
[0005] Ageing, chronic exposure to adverse environmental factors,
malnutrition, fatigue, etc., can change the visual appearance,
physical properties, or physiological functions of skin in ways
that are considered visually undesirable. The most notable and
obvious changes include the development of fine lines and wrinkles,
loss of elasticity, increased sagging, loss of firmness, loss of
color evenness or tone, coarse surface texture, and mottled
pigmentation. Less obvious but measurable changes which occur as
skin ages or endures chronic environmental insult include a general
reduction in cellular and tissue vitality, reduction in cell
replication rates, reduced cutaneous blood flow, reduced moisture
content, accumulated errors in structure and function, alterations
in the normal regulation of common biochemical pathways, and a
reduction in the skin's ability to remodel and repair itself. Many
of the alterations in appearance and function of the skin are
caused by changes in the outer epidermal layer of the skin, while
others are caused by changes in the lower dermis.
[0006] Previous attempts to improve the visual appearance of skin
with known skin active-ingredients have been shown to have various
drawbacks such as skin irritation and prolonged recovery
periods.
[0007] Maintaining moisture of the skin and/or hair helps overcome
some unwanted changes in skin and hair. However, maintaining
moisture of the skin can be difficult. This is even true for
subjects with oily skin (oily skin type). Exposure to chemicals,
solvents, washing, cosmetics, fabrics, or dry environments are some
of the many ways that skin can lose moisture.
[0008] Skin and hair can lose moisture as a result of cleansing
and/or freshening the skin and hair. Skin and hair cleansing and/or
freshening compositions are typically applied to skin and/or hair
and rinsed-off with water (e.g., rinse-off product), robbing the
skin of natural oils and lipids. Further, cleansing and freshening
compositions oftentimes have ingredients that can be caustic to the
surfaces to be cleansed. For instance, many types of cleansers and
fresheners use certain surfactants that can cause skin
irritation.
[0009] Cosmetics, including makeup foundations and masks, can cause
drying of the skin. Foundations are typically applied to skin and
left on the skin so that additional makeup may be applied or to
hide the appearance of unwanted blemishes or colors. Some problems
associated with foundations include skin irritation, stability,
lack of adequate effectiveness, difficulty in applying to skin, and
drying of the skin. Masks are typically applied to skin and left on
the skin for a period of time to allow the claimed benefits of the
mask to occur. Problems associated with masks include skin
irritation, stability, lack of adequate effectiveness, difficulty
in applying to skin, and drying of the skin. Many masks also
exfoliate the skin, which can cause or exasperate irritation,
sensitivity, and dryness.
[0010] Moisturizers are complex mixtures of chemical agents
specially designed to make the external layers of the skin
(epidermis) softer and more pliable. They increase the skin's
hydration (water content) by reducing evaporation. Naturally
occurring skin lipids and sterols, as well as artificial or natural
oils, humectants, emollients, lubricants, etc., may be part of the
composition of commercial skin moisturizers. They usually are
available as commercial products for cosmetic and therapeutic uses,
but can also be made at home using common pharmacy ingredients.
However, moisturizers are not perfect. Some problems associated
with moisturizers include unpleasant tactile properties (e.g.,
heavy, greasy, or sticky feel), instability, skin-irritation, or
insufficient moisturization capabilities.
SUMMARY OF THE INVENTION
[0011] The inventors determined that a combination of compounds,
compositions, and extracts that have therapeutic benefits. In
particular, the inventors identified a combination of ingredients,
including hydrolyzed algin, zinc sulfate, and saccharide isomerate,
that work to moisturize and improve the appearance and condition of
the skin and/or hair. In particular aspects, the saccharide
isomerate may contain an exopolysaccharide synthesized by Vibrio
alginolyticus, capable of increasing production of filaggrin,
increasing skin moisture, increasing production of occluding,
inhibiting TNF.alpha. production, and/or preventing oxidative
damage. In particular aspects, the hydrolyzed algin is an anionic
polysaccharide produced by Laminaria digitate and when combined
with zinc sulfate is capable of inhibiting PPAR-.gamma. activity,
inhibiting MMP1 activity, inhibiting MMP9 activity, and/or
inhibiting elastase activity. The present invention overcomes
deficiencies in the art by providing stable moisturizer, mask,
foundation, freshener, and cleanser compositions that can also
effectively increase filaggrin production, increase skin moisture,
increase occludin production, inhibit TNF.alpha. production,
prevent oxidative damage, inhibit PPAR-.gamma. activity, inhibit
MMP1 activity, inhibit MMP9 activity, and inhibit elastase
activity.
[0012] In some embodiments, there is disclosed a topical
composition. In some aspects, the topical composition includes any
one of, any combination of, or all of hydrolyzed algin, zinc
sulfate, saccharide isomerate, and a dermatologically acceptable
vehicle. The amounts of the ingredients within the composition can
vary (e.g., amounts can be as low as 0.000001% to as high as 98%
w/w or any range therein). In some aspects, the composition
contains an effective amount of saccharide isomerate capable of
increasing production of filaggrin, increasing skin moisture,
increasing production of occluding, inhibiting TNF.alpha.
production, and/or preventing oxidative damage. In some aspects,
the composition contains an effective amount of hydrolyzed algin
and zinc sulfate capable of inhibiting PPAR-.gamma. activity,
inhibiting MMP1 activity, inhibiting MMP9 activity, and/or
inhibiting elastase activity. In some aspects, the saccharide
isomerate comprises an exopolysaccharide synthesized by Vibrio
alginolyticus. In some aspects, the hydrolyzed algin extract
comprises an anionic polysaccharide synthesized by Laminaria
digitate. In some aspects the composition includes: 0.0001% to 2%
w/w of saccharide isomerate, 0.001% to 2% w/w of hydrolyzed algin,
and 0.0001% to 1% w/w of zinc sulfate. In some aspects, the
dermatologically acceptable vehicle contains or is water. In some
aspects, the composition includes 30% to 98% w/w of water. In some
aspects, the composition is formulated to moisturize skin and/or
hair. In some aspects, the composition is formulated to moisturize
oily skin and/or hair. In some aspects, the composition is
formulated as a moisturizer, a mask, a foundation, a freshener,
and/or a cleanser. The composition may further comprise one or more
ingredients described herein. For example, the composition may
comprise one or more additional ingredients selected from one or
more conditioning agents, moisturizing agents, pH adjusters,
structuring agents, inorganic salts, and preservatives.
[0013] In another aspect, disclosed is a moisturizer. In some
aspects, the topical composition above further includes any one of,
any combination of, or all of glycerin, cetearyl ethylhexanoate,
pentylene glycol, biosaccharide gum-1, dimethicone, silica,
cyclopentasiloxane, and ammonium acryloyldimethyltaurate/VP
copolymer. The amounts of the ingredients within the composition
can vary (e.g., amounts can be as low as 0.000001% to as high as
98% w/w or any range therein). In some aspects the composition
includes: 15% to 50% w/w of glycerin, 1% to 15% w/w of cetearyl
ethylhexanoate, 1% to 10% w/w of pentylene glycol, 1% to 10% w/w of
biosaccharide gum-1, 1% to 10% w/w of dimethicone, 0.5% to 5% w/w
of silica, 0.5% to 5% w/w of cyclopentasiloxane, and 0.5% to 5% w/w
of ammonium acryloyldimethyltaurate/VP copolymer. In some aspects,
the composition further includes: phenoxyethanol, PEG-12
dimethicone, caprylyl glycol, chlorphenesin, dimethiconol, and
dipotassium glycyrrhizate. In some aspects, the composition
includes: 0.1% to 3% w/w of phenoxyethanol, 0.1% to 3% w/w of
PEG-12 dimethicone, 0.05% to 1% w/w of caprylyl glycol, 0.05% to
0.5% w/w of chlorphenesin, 0.01% to 0.5% w/w of dimethiconol, and
0.01% to 0.5% w/w of dipotassium glycyrrhizate. In some aspects,
the composition further includes Opuntia tuna fruit extract. In
some aspects, the composition includes 0.0001% to 0.1% w/w of
Opuntia tuna fruit extract. In some aspects, the composition is
formulated as a moisturizer.
[0014] In yet another aspect, disclosed is a mask. In some aspects,
the topical composition above further includes kaolin, C12-15
alcohols benzoate, titanium dioxide, propylene glycol, magnesium
aluminum silicate, TEA-lauryl sulfate, xanthan gum, and
phenoxyethanol. The amounts of the ingredients within the
composition can vary (e.g., amounts can be as low as 0.000001% to
as high as 98% w/w or any range therein). In some aspects, the
composition includes 25% to 45% w/w of kaolin, 1% to 10% w/w of
C12-15 alcohols benzoate, 1% to 10% w/w of titanium dioxide, 1% to
10% w/w of propylene glycol, 0.5% to 5% w/w of magnesium aluminum
silicate, 0.5% to 5% w/w of TEA-lauryl sulfate, 0.1% to 3% w/w of
xanthan gum, and 0.1% to 3% w/w of phenoxyethanol. In some aspects,
the composition further includes benzyl alcohol. In some aspects
the composition includes 0.1% to 3% w/w of benzyl alcohol. In some
aspects, the composition further includes caprylyl alcohol. In some
aspects, the composition includes 0.1% to 3% w/w of caprylyl
alcohol. In some aspects, the composition further includes Opuntia
tuna fruit extract. In some aspects, the composition includes
0.0001% to 0.1% w/w of Opuntia tuna fruit extract. In some aspects,
the composition is formulated as a mask.
[0015] In one aspect, disclosed is a foundation. In some aspects,
the topical composition above further includes any one of, any
combination of, or all of titanium dioxide, cyclopentasiloxane,
C12-15 alkyl benzoate, octinoxate, methyl methacrylate
crosspolymer, neopentyl glycol dicaprate, dipropylene glycol,
butylene glycol, C14-22 alcohols, oxybenzone, iron oxides, silica,
glycerin, and stearic acid. The amounts of the ingredients within
the composition can vary (e.g., amounts can be as low as 0.000001%
to as high as 98% w/w or any range therein). In some aspects, the
composition includes 1% to 10% w/w of titanium dioxide, 1% to 10%
w/w of cyclopentasiloxane, 1% to 10% w/w of C12-15 alkyl benzoate,
1% to 10% w/w of octinoxate, 1% to 10% w/w of methyl methacrylate
crosspolymer, 1% to 10% w/w of neopentyl glycol dicaprate, 0.5% to
5% w/w of dipropylene glycol, 0.5% to 5% w/w of butylene glycol,
0.5% to 5% w/w of C14-22 alcohols, 0.5% to 5% w/w of oxybenzone,
0.1% to 3% w/w of iron oxides, 0.1% to 3% w/w of silica, 0.1% to 3%
w/w of glycerin, and 0.1% to 3% w/w of stearic acid. In some
aspects, the composition further includes: benzyl alcohol, C12-20
alkyl glucoside, hydroxyethyl acrylate/sodium acryloyldimethyl
taurate copolymer, triethanolamine, isohexadecane, xanthan gum,
salicylic acid, and disodium EDTA. In some aspects, the composition
includes 0.1% to 3% w/w of benzyl alcohol, 0.1% to 3% w/w of C12-20
alkyl glucoside, 0.1% to 3% w/w of hydroxyethyl acrylate/sodium
acryloyldimethyl taurate copolymer, 0.1% to 3% w/w of
triethanolamine, 0.1% to 3% w/w of isohexadecane, 0.01% to 1% w/w
of xanthan gum, 0.01% to 1% w/w of salicylic acid, and 0.01% to 1%
w/w of disodium EDTA. In some aspects, the composition further
includes Opuntia tuna fruit extract. In some aspects, the
composition includes 0.0001% to 0.1% w/w of Opuntia tuna fruit
extract. In some aspects, the composition is formulated as a
foundation.
[0016] In another aspect, disclosed is a freshener. In some
aspects, the topical composition above further includes any one of,
any combination of, or all of butylene glycol and glycerin. The
amounts of the ingredients within the composition can vary (e.g.,
amounts can be as low as 0.000001% to as high as 98% w/w or any
range therein). In some aspects, the composition includes: 1% to
10% w/w of butylene glycol and 0.1% to 3% w/w of glycerin. In some
aspects, the composition further includes: caprylyl glycol,
PPG-5-ceteth-20, 1,2-hexanediol, and disodium EDTA. In some
aspects, the composition includes: 0.1% to 1.5% w/w of caprylyl
glycol, 0.1% to 1.5% w/w of PPG-5-ceteth-20, 0.1% to 1.5% w/w of
1,2-hexanediol, and 0.01% to 1% w/w of disodium EDTA. In some
aspects the composition further includes Opuntia tuna fruit
extract. In some aspects, the composition includes 0.0001% to 0.1%
w/w of Opuntia tuna fruit extract. In some aspects, the composition
is formulated as a freshener.
[0017] In another aspect, disclosed is a cleanser. In some aspects,
the topical composition above further includes any one of, any
combination of, or all of sodium cocoyl glycinate and
cocamidopropyl betaine. In some aspects, the composition further
includes hydroxyethylcellulose and polyglyceryl-4 caprate. In some
aspects, the topical composition above further includes any one of,
any combination of, or all of TEA-lauryl sulfate and at least two
of sodium C14-16 olefin sulfonate, cocamidopropyl hydroxysultaine,
sodium methyl cocoyl taurate, and/or sodium cocoyl glycinate. In
some aspects, the composition further includes TEA-lauryl sulfate,
sodium methyl cocoyl taurate, sodium chloride, and hydroxypropyl
cyclodextrin. In some aspects, the composition includes 1% to 10%
w/w of TEA-lauryl sulfate, 0.5% to 5% w/w of sodium methyl cocoyl
taurate, 0.1% to 1.5% w/w of sodium chloride, and 0.01% to 1% w/w
of hydroxypropyl cyclodextrin. In some aspects, the composition
further includes PEG-8, sorbitol, glycerin, hexylene glycol,
PEG-32, phenoxyethanol, chlorphenesin, disodium EDTA, and salicylic
acid. In some aspects, the composition includes 1% to 10% w/w of
PEG-8, 0.5% to 5% w/w of sorbitol, 0.5% to 5% w/w of glycerin, 0.1%
to 3% w/w of hexylene glycol, 0.1% to 3% w/w of PEG-32, 0.1% to 3%
w/w of phenoxyethanol, 0.01% to 1% w/w of chlorphenesin, 0.01% to
1% w/w of disodium EDTA, and 0.01% to 1% w/w of salicylic acid. In
some aspects, the composition further includes potassium hydroxide.
In some aspects, the composition further includes Opuntia tuna
fruit extract. The amounts of the ingredients within the
composition can vary (e.g., amounts can be as low as 0.000001% to
as high as 98% w/w or any range therein). In some aspects, the
composition includes 0.0001% to 0.1% w/w of Opuntia tuna fruit
extract. In some aspects, the composition is formulated as a
cleanser.
[0018] The composition may further comprise one or more ingredients
described herein. For example, the composition may comprise one or
more additional ingredients selected from one or more conditioning
agents, moisturizing agents, pH adjusters, structuring agents,
inorganic salts, and preservatives.
[0019] Methods of use for the compositions disclosed herein are
also disclosed. In some aspects, the compositions disclosed are
applied to skin and/or hair by applying the composition to skin
and/or hair and leaving the composition on the skin and/or hair. In
some aspects, the compositions disclosed are applied to skin and/or
hair by applying the composition to skin and/or hair and removing
the composition from the skin and/or hair. In some aspects, the
compositions disclosed are removed immediately after applying the
composition to up to 16 hours after applying the composition. In
some embodiments, the compositions disclosed are used to moisturize
skin and/or hair by applying the composition to skin and/or hair.
In some embodiments, the compositions disclosed are used to remove
residue from skin and/or hair by applying the composition to skin
and/or hair and removing the composition from the skin and/or hair.
In some embodiments, the compositions disclosed are used to cleanse
skin and/or hair by applying the composition to skin and/or hair
and removing the composition from the skin and/or hair.
[0020] Methods of use for the compositions are disclosed where in
some embodiments, the compositions disclosed increase filaggrin
production by applying the composition to skin, wherein filaggrin
production is increased. In some embodiments, the compositions
disclosed moisturize the skin by applying the composition to skin,
wherein skin moisture is increased. In some embodiments, the
compositions disclosed increase production of occludin by applying
the composition to skin, wherein occludin production is increased.
In some embodiments, the compositions disclosed inhibit production
of TNF.alpha. by applying the composition to skin, wherein
TNF.alpha. production is inhibited. In some embodiments, the
compositions disclosed prevent oxidative damage by applying the
composition to skin and/or hair, wherein oxidative damage is
prevented. In some embodiments, the compositions disclosed inhibit
PPAR-.gamma. activity by applying the composition to skin, wherein
PPAR-.gamma. activity is inhibited. In some embodiments, the
compositions disclosed inhibit MMP1 by applying the composition to
skin, wherein MMP1 is inhibited. In some embodiments, the
compositions disclosed inhibit MMP9 by applying the composition to
skin, wherein MMP9 is inhibited. In some embodiments, the
compositions disclosed inhibit elastase by applying the composition
to skin, wherein elastase is inhibited. In some embodiments, the
compositions disclosed are used to treat a subject in need thereof
by applying the composition to skin, wherein at least one of
filaggrin production is increased, skin moisture is increased,
occludin production is increased, TNF.alpha. production is
inhibited, and oxidative damage is prevented, and wherein at least
one of PPAR-.gamma. activity is inhibited, MMP1 is inhibited, MMP9
is inhibited, and elastase is inhibited.
[0021] In some aspects, the compositions are formulated as a
topical skin composition. The composition can have a
dermatologically acceptable vehicle or carrier for the compounds,
compositions and extracts. The composition can further include a
moisturizing agent or a humectant, a surfactant, a silicone
containing compounds, a UV agent, an oil, and/or other ingredients
identified in this specification or those known in the art. The
composition can be a lotion, cream, gel, serum, emulsion (e.g.,
oil-in-water, water-in-oil, silicone-in-water, water-in-silicone,
water-in-oil-in-water, oil-in-water-in-oil,
oil-in-water-in-silicone, etc.), solutions (e.g., aqueous or
hydro-alcoholic solutions), anhydrous bases (e.g., lipstick or a
powder), ointments, milk, paste, aerosol, solid forms, eye jellies,
etc. The composition can be in powdered form (e.g., dried,
lyophilized, particulate, etc.). The composition can be formulated
for topical skin application at least 1, 2, 3, 4, 5, 6, 7, or more
times a day during use. In other aspects of the present invention,
compositions can be storage stable or color stable, or both. It is
also contemplated that the viscosity of the composition can be
selected to achieve a desired result, e.g., depending on the type
of composition desired, the viscosity of such composition can be
from about 1 cps to well over 1 million cps or any range or integer
derivable therein (e.g., 2 cps, 3, 4, 5, 6, 7, 8, 9, 10, 20, 30,
40, 50, 60, 70, 80, 90, 100, 200, 300, 400, 500, 600, 700, 800,
900, 1000, 2000, 3000, 4000, 5000, 6000, 7000, 8000, 9000, 10000,
20000, 30000, 40000, 50000, 60000, 70000, 80000, 90000, 100000,
200000, 300000, 400000, 500000, 600000, 700000, 800000, 900000,
1000000, 2000000, 3000000, 4000000, 5000000, 10000000, cps, etc.,
as measured on a Brookfield Viscometer using a TC spindle at 2.5
rpm at 25.degree. C.).
[0022] In some instances, the compositions can also be modified to
have a desired oxygen radical absorbance capacity (ORAC) value. In
certain non-limiting aspects, the compositions of the present
invention or the component or extracts thereof identified
throughout this specification can be modified to have an ORAC value
per mg of at least about 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13,
14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30,
35, 40, 45, 50, 55, 60, 70, 80, 90, 95, 100, 200, 300, 400, 500,
600, 700, 800, 900, 1000, 2000, 3000, 4000, 5000, 6000, 7000, 8000,
9000, 10000, 15000, 20000, 30000, 50000, 100000 or more or any
range derivable therein.
[0023] The compositions in non-limiting aspects can have a pH of
about 6 to about 9. In other aspects, the pH can be 1, 2, 3, 4, 5,
6, 7, 8, 9, 10, 11, 12, 13, or 14. The compositions can include a
triglyceride. Non-limiting examples include small, medium, and
large chain triglycerides. In certain aspects, the triglyceride is
a medium chain triglyceride (e.g., caprylic capric triglyceride).
In some instances, the compositions can also include preservatives.
Non-limiting examples of preservatives include methylparaben,
propylparaben, or a mixture of methylparaben and propylparaben.
[0024] In some aspects, compositions can have UVA and UVB
absorption properties. The compositions can have an sun protection
factor (SPF) of 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 20,
25, 30, 35, 40, 45, 50, 55, 60, or more, or any integer or
derivative therein. The compositions can be sunscreen lotions,
sprays, or creams.
[0025] The compositions can also include any one of, any
combination of, or all of the following additional ingredients:
water, a chelating agent, a moisturizing agent, a preservative, a
thickening agent, a silicone containing compound, an essential oil,
a structuring agent, a vitamin, a pharmaceutical ingredient, or an
antioxidant, or any combination of such ingredients or mixtures of
such ingredients. In certain aspects, the composition can include
at least two, three, four, five, six, seven, eight, nine, ten, or
all of these additional ingredients identified in the previous
sentence. Non-limiting examples of these additional ingredients are
identified throughout this specification and are incorporated into
this section by reference. The amounts of such ingredients can
range from 0.0001% to 99.9% by weight or volume of the composition,
or any integer or range in between as disclosed in other sections
of this specification, which are incorporated into this paragraph
by reference.
[0026] Kits that include the compositions are also contemplated. In
certain embodiments, the composition is comprised in a container.
The container can be a bottle, dispenser, or package. The container
can dispense a pre-determined amount of the composition. In certain
aspects, the compositions is dispensed in a spray, mist, dollop, or
liquid. The container can include indicia on its surface. The
indicia can be a word, an abbreviation, a picture, or a symbol.
[0027] It is also contemplated that the compositions disclosed
throughout this specification can be used as a leave-on or
rinse-off composition. By way of example, a leave-on composition
can be one that is topically applied to skin and remains on the
skin for a period of time (e.g., at least 5, 6, 7, 8, 9, 10, 20, or
30 minutes, or at least 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13,
14, 15, 16, 17, 18, 19, 20, 21, 22, 23 or 24 hours, or overnight or
throughout the day). Alternatively, a rinse-off composition can be
a product that is intended to be applied to the skin and then
removed or rinsed from the skin (e.g., with water) within a period
of time such as less than 5, 4, 3, 2, or 1 minute. An example of a
rinse of composition can be a skin cleanser, shampoo, conditioner,
or soap. An example of a leave-on composition can be a skin
moisturizer, sunscreen, mask, overnight cream, or a day cream.
[0028] It is contemplated that any embodiment discussed in this
specification can be implemented with respect to any method or
composition of the invention, and vice versa. Furthermore,
compositions of the invention can be used to achieve methods of the
invention.
[0029] In some embodiments, compositions can be pharmaceutically or
cosmetically elegant or can have pleasant tactile properties.
"Pharmaceutically elegant," "cosmetically elegant," and/or
"pleasant tactile properties" describes a composition that has
particular tactile properties which feel pleasant on the skin
(e.g., compositions that are not too watery or greasy, compositions
that have a silky texture, compositions that are non-tacky or
sticky, etc.). Pharmaceutically or cosmetically elegant can also
relate to the creaminess or lubricity properties of the composition
or to the moisture retaining properties of the composition.
[0030] Also contemplated is a product comprising the composition.
In non-limiting aspects, the product can be a cosmetic product. The
cosmetic product can be those described in other sections of this
specification or those known to a person of skill in the art.
Non-limiting examples of products include a moisturizer, a cream, a
lotion, a skin softener, a gel, a wash, a foundation, a night
cream, a lipstick, a cleanser, a toner, a sunscreen, a mask, an
anti-aging product, a deodorant, an antiperspirant, a perfume, a
cologne, etc.
[0031] Also disclosed are the following Embodiments 1 to 59 of the
present invention. Embodiment 1 is a method of treating a subject
in need thereof comprising applying a topical composition
comprising saccharide isomerate, hydrolyzed algin, zinc sulfate,
and a dermatologically acceptable vehicle to skin, wherein at least
one of filaggrin production is increased, skin moisture is
increased, occludin production is increased, TNF.alpha. production
is inhibited, oxidative damage is prevented, PPAR-.gamma. activity
is inhibited, MMP1 is inhibited, MMP9 is inhibited, or elastase is
inhibited. Embodiment 2 is the method of Embodiment 1, wherein at
least one of filaggrin production is increased, skin moisture is
increased, occludin production is increased, TNF.alpha. production
is inhibited, or oxidative damage is prevented, and wherein at
least one of PPAR-.gamma. activity is inhibited, MMP1 is inhibited,
MMP9 is inhibited, or elastase is inhibited. Embodiment 3 is the
method of any of Embodiments 1 and 2, wherein the saccharide
isomerate increases production of filaggrin, increases skin
moisture, increases production of occluding, inhibits TNF.alpha.
production, and/or prevents oxidative damage. Embodiment 4 is the
method of any of Embodiments 1 to 3, wherein the hydrolyzed algin
and zinc sulfate inhibit PPAR-.gamma. activity, inhibit MMP1
activity, inhibit MMP9 activity, and/or inhibit elastase activity.
Embodiment 5 is the method of any of Embodiments 1 to 4, wherein
the saccharide isomerate comprises an exopolysaccharide synthesized
by Vibrio alginolyticus. Embodiment 6 is the method of any of
Embodiments 1 to 5, wherein the hydrolyzed algin extract comprises
an anionic polysaccharide synthesized by Laminaria digitate.
Embodiment 7 is the method of any of Embodiments 1 to 6, wherein
the composition comprises 0.0001% to 2% w/w of saccharide
isomerate, 0.001% to 2% w/w of hydrolyzed algin, and 0.0001% to 1%
w/w of zinc sulfate. Embodiment 8 is the method of any of
Embodiments 1 to 7, wherein the composition is formulated as at
least one of a moisturizer, a mask, a foundation, a freshener,
and/or a cleanser. Embodiment 9 is the method of any of Embodiments
1 to 8, wherein the wherein the dermatologically acceptable vehicle
comprises water. Embodiment 10 is the method of Embodiment 9,
wherein the composition comprises 30% to 98% w/w of water.
Embodiment 11 is a topical composition comprising saccharide
isomerate, hydrolyzed algin, zinc sulfate, and a dermatologically
acceptable vehicle, wherein the composition is capable of
moisturizing at least one of skin and/or hair, wherein the
saccharide isomerate comprises an exopolysaccharide synthesized by
Vibrio alginolyticus, and wherein the hydrolyzed algin extract
comprises an anionic polysaccharide synthesized by Laminaria
digitate. Embodiment 12 is the composition of Embodiment 11,
wherein the composition comprises an effective amount of saccharide
isomerate capable of increasing production of filaggrin, increasing
skin moisture, increasing production of occluding, inhibiting
TNF.alpha. production, and/or preventing oxidative damage.
Embodiment 13 is the composition of any of Embodiments 11 to 12,
wherein the composition comprises an effective amount of hydrolyzed
algin and zinc sulfate capable of inhibiting PPAR-.gamma. activity,
inhibiting MMP1 activity, inhibiting MMP9 activity, and/or
inhibiting elastase activity. Embodiment 14 is the composition of
any of Embodiments 11 to 13, wherein the composition is formulated
to moisturize at least one of oily skin and/or oily hair.
Embodiment 15 is the composition of any of Embodiments 11 to 14,
wherein the composition comprises 0.0001% to 2% w/w of saccharide
isomerate, 0.001% to 2% w/w of hydrolyzed algin, and 0.0001% to 1%
w/w of zinc sulfate. Embodiment 16 is the composition of any of
Embodiments 11 to 15, wherein the composition is formulated as at
least one of a moisturizer, a mask, a foundation, a freshener,
and/or a cleanser. Embodiment 17 is the composition of any of
Embodiments 11 to 16, wherein the dermatologically acceptable
vehicle comprises water. Embodiment 18 is the composition of any of
Embodiments 11 to 17, wherein the composition comprises 30% to 98%
w/w of water. Embodiment 19 is the composition of any of
Embodiments 11 to 18, wherein the composition further comprises:
glycerin; cetearyl ethylhexanoate; pentylene glycol; biosaccharide
gum-1; dimethicone; silica; cyclopentasiloxane; and ammonium
acryloyldimethyltaurate/VP copolymer. Embodiment 20 is the
composition of Embodiment 19, wherein the composition comprises:
15% to 50% w/w of glycerin; 1% to 15% w/w of cetearyl
ethylhexanoate; 1% to 10% w/w of pentylene glycol; 1% to 10% w/w of
biosaccharide gum-1; 1% to 10% w/w of dimethicone; 0.5% to 5% w/w
of silica; 0.5% to 5% w/w of cyclopentasiloxane; and 0.5% to 5% w/w
of ammonium acryloyldimethyltaurate/VP copolymer. Embodiment 21 is
the composition of any of Embodiments 11 to 20, wherein the
composition further comprises: phenoxyethanol; PEG-12 dimethicone;
caprylyl glycol; chlorphenesin; dimethiconol; and dipotassium
glycyrrhizate. Embodiment 22 is the composition of Embodiment 21,
wherein the composition comprises: 0.1% to 3% w/w of
phenoxyethanol; 0.1% to 3% w/w of PEG-12 dimethicone; 0.05% to 1%
w/w of caprylyl glycol; 0.05% to 0.5% w/w of chlorphenesin; 0.01%
to 0.5% w/w of dimethiconol; and 0.01% to 0.5% w/w of dipotassium
glycyrrhizate. Embodiment 23 is the composition of any of
Embodiments 11 to 22, wherein the composition further comprises
Opuntia tuna fruit extract. Embodiment 24 is the composition of
Embodiment 23, wherein the composition comprises 0.0001% to 0.1%
w/w of Opuntia tuna fruit extract. Embodiment 25 is the composition
of any of Embodiments 11 to 24, wherein the composition is
formulated as a moisturizer. Embodiment 26 is the composition of
any of Embodiments 11 to 18, wherein the composition further
comprises: kaolin; C12-15 alcohols benzoate; titanium dioxide;
propylene glycol; magnesium aluminum silicate; TEA-lauryl sulfate;
xanthan gum; and phenoxyethanol. Embodiment 27 is the composition
of Embodiment 26, wherein the composition comprises: 25% to 45% w/w
of kaolin; 1% to 10% w/w of C12-15 alcohols benzoate; 1% to 10% w/w
of titanium dioxide; 1% to 10% w/w of propylene glycol; 0.5% to 5%
w/w of magnesium aluminum silicate; 0.5% to 5% w/w of TEA-lauryl
sulfate; 0.1% to 3% w/w of xanthan gum; and 0.1% to 3% w/w of
phenoxyethanol. Embodiment 28 is the composition of any of
Embodiments 26 to 27, wherein the composition further comprises
benzyl alcohol. Embodiment 29 is the composition of Embodiment 28,
wherein the composition comprises 0.1% to 3% w/w of benzyl alcohol.
Embodiment 30 is the composition of any of Embodiments 26 to 29,
wherein the composition further comprises caprylyl alcohol.
Embodiment 31 is the composition of Embodiment 30, wherein the
composition comprises 0.1% to 3% w/w of caprylyl alcohol.
Embodiment 32 is the composition of any of Embodiments 26 to 31,
wherein the composition further comprises Opuntia tuna fruit
extract. Embodiment 33 is the composition of Embodiment 32, wherein
the composition comprises 0.0001% to 0.1% w/w of Opuntia tuna fruit
extract. Embodiment 34 is the composition of any of Embodiments 26
to 33, wherein the composition is formulated as a mask. Embodiment
35 is the composition of any of Embodiments 11 to 18, wherein the
composition further comprises: titanium dioxide;
cyclopentasiloxane; C12-15 alkyl benzoate; octinoxate; methyl
methacrylate crosspolymer; neopentyl glycol dicaprate; dipropylene
glycol; butylene glycol; C14-22 alcohols; oxybenzone; iron oxides;
silica; glycerin; and stearic acid. Embodiment 36 is the
composition of Embodiment 35, wherein the composition comprises: 1%
to 10% w/w of titanium dioxide; 1% to 10% w/w of
cyclopentasiloxane; 1% to 10% w/w of C12-15 alkyl benzoate; 1% to
10% w/w of octinoxate; 1% to 10% w/w of methyl methacrylate
crosspolymer; 1% to 10% w/w of neopentyl glycol dicaprate; 0.5% to
5% w/w of dipropylene glycol; 0.5% to 5% w/w of butylene glycol;
0.5% to 5% w/w of C14-22 alcohols; 0.5% to 5% w/w of oxybenzone;
0.1% to 3% w/w of iron oxides; 0.1% to 3% w/w of silica; 0.1% to 3%
w/w of glycerin; and 0.1% to 3% w/w of stearic acid. Embodiment 37
is the composition of any of Embodiments 35 to 36, wherein the
composition further comprises: benzyl alcohol; C12-20 alkyl
glucoside; hydroxyethyl acrylate/sodium acryloyldimethyl taurate
copolymer; triethanolamine; isohexadecane; xanthan gum; salicylic
acid; and disodium EDTA. Embodiment 38 is the composition of
Embodiment 37, wherein the composition comprises: 0.1% to 3% w/w of
benzyl alcohol; 0.1% to 3% w/w of C12-20 alkyl glucoside; 0.1% to
3% w/w of hydroxyethyl acrylate/sodium acryloyldimethyl taurate
copolymer; 0.1% to 3% w/w of triethanolamine; 0.1% to 3% w/w of
isohexadecane; 0.01% to 1% w/w of xanthan gum; 0.01% to 1% w/w of
salicylic acid; and 0.01% to 1% w/w of disodium EDTA. Embodiment 39
is the composition of any of Embodiments 35 to 38, wherein the
composition further comprises Opuntia tuna fruit extract.
Embodiment 40 is the composition of Embodiment 39, wherein the
composition comprises 0.0001% to 0.1% w/w of Opuntia tuna fruit
extract. Embodiment 41 is the composition of any of Embodiments 35
to 40, wherein the composition is formulated as a foundation.
Embodiment 42 is the composition of any of Embodiments 11 to 18,
wherein the composition further comprises: butylene glycol; and
glycerin. Embodiment 43 is the composition of Embodiment 42,
wherein the composition comprises: 1% to 10% w/w of butylene
glycol; and 0.1% to 3% w/w of glycerin. Embodiment 44 is the
composition of any of Embodiments 42 to 43, wherein the composition
further comprises: caprylyl glycol; PPG-5-ceteth-20;
1,2-hexanediol; and disodium EDTA. Embodiment 45 is the composition
of Embodiment 44, wherein the composition comprises: 0.1% to 1.5%
w/w of caprylyl glycol; 0.1% to 1.5% w/w of PPG-5-ceteth-20; 0.1%
to 1.5% w/w of 1,2-hexanediol; and 0.01% to 1% w/w of disodium
EDTA. Embodiment 46 is the composition of any of Embodiments 42 to
45, wherein the composition further comprises Opuntia tuna fruit
extract. Embodiment 47 is the composition of Embodiment 46, wherein
the composition comprises 0.0001% to 0.1% w/w of Opuntia tuna fruit
extract. Embodiment 48 is the composition of any of Embodiments 42
to 47, wherein the composition is formulated as a freshener.
Embodiment 49 is the composition of any of Embodiments 11 to 18,
wherein the composition further comprises: sodium cocoyl glycinate;
and cocamidopropyl betaine. Embodiment 50 is the composition of
Embodiment 49, wherein the composition further comprises:
hydroxyethylcellulose; and polyglyceryl-4 caprate. Embodiment 51 is
the composition of any of Embodiments 11 to 18, wherein the
composition further comprises: TEA-lauryl sulfate; and at least two
of sodium C14-16 olefin sulfonate, cocamidopropyl hydroxysultaine,
sodium methyl cocoyl taurate, and sodium cocoyl glycinate.
Embodiment 52 is the composition of any of Embodiments 11 to 18,
wherein the composition further comprises: TEA-lauryl sulfate;
sodium methyl cocoyl taurate; sodium chloride; and hydroxypropyl
cyclodextrin. Embodiment 53 is the composition of Embodiment 52,
wherein the composition comprises: 1% to 10% w/w of TEA-lauryl
sulfate; 0.5% to 5% w/w of sodium methyl cocoyl taurate; 0.1% to
1.5% w/w of sodium chloride; and 0.01% to 1% w/w of hydroxypropyl
cyclodextrin. Embodiment 54 is the composition of any of
Embodiments 49 to 53, wherein the composition further comprises:
PEG-8; sorbitol; glycerin; hexylene glycol; PEG-32; phenoxyethanol;
chlorphenesin; disodium EDTA; and salicylic acid. Embodiment 55 is
the composition of Embodiment 54, wherein the composition
comprises: 1% to 10% w/w of PEG-8; 0.5% to 5% w/w of sorbitol; 0.5%
to 5% w/w of glycerin; 0.1% to 3% w/w of hexylene glycol; 0.1% to
3% w/w of PEG-32; 0.1% to 3% w/w of phenoxyethanol; 0.01% to 1% w/w
of chlorphenesin; 0.01% to 1% w/w of disodium EDTA; and 0.01% to 1%
w/w of salicylic acid. Embodiment 56 is the composition of
Embodiment 54, wherein the composition further comprises potassium
hydroxide. Embodiment 57 is the composition of any of Embodiments
49 to 56, wherein the composition further comprises Opuntia tuna
fruit extract. Embodiment 58 is the composition of Embodiment 57,
wherein the composition comprises 0.0001% to 0.1% w/w of Opuntia
tuna fruit extract. Embodiment 59 is the composition of any of
Embodiments 49 to 58, wherein the composition is formulated as a
cleanser.
[0032] "Topical application" means to apply or spread a composition
onto the surface of lips or keratinous tissue. "Topical skin
composition" includes compositions suitable for topical application
on lips or keratinous tissue. Such compositions are typically
dermatologically-acceptable in that they do not have undue
toxicity, incompatibility, instability, allergic response, and the
like, when applied to lips or skin. Topical skin care compositions
of the present invention can have a selected viscosity to avoid
significant dripping or pooling after application to skin.
[0033] "Keratinous tissue" includes keratin-containing layers
disposed as the outermost protective covering of mammals and
includes, but is not limited to, lips, skin, hair and nails.
[0034] The term "about" or "approximately" are defined as being
close to as understood by one of ordinary skill in the art, and in
one non-limiting embodiment the terms are defined to be within 10%,
preferably within 5%, more preferably within 1%, and most
preferably within 0.5%.
[0035] The term "substantially" and its variations are defined as
being largely but not necessarily wholly what is specified as
understood by one of ordinary skill in the art, and in one
non-limiting embodiment substantially refers to ranges within 10%,
within 5%, within 1%, or within 0.5%.
[0036] The terms "inhibiting" or "reducing" or any variation of
these terms includes any measurable decrease or complete inhibition
to achieve a desired result. The terms "promote" or "increase" or
any variation of these terms includes any measurable increase or
production of a protein or molecule (e.g., matrix proteins such as
fibronectin, laminin, collagen, or elastin or molecules such as
hyaluronic acid) to achieve a desired result.
[0037] "Treating" or any variation of this term includes any
measurable improvement in a disease, condition, or symptom that is
being treated or is associated with the disease, condition, or
symptom being treated.
[0038] "Preventing" or any variation of this term means to slow,
stop, or reverse progression toward a result. The prevention may be
any slowing of the progression toward the result.
[0039] The term "effective," as that term is used in the
specification and/or claims, means adequate to accomplish a
desired, expected, or intended result.
[0040] The use of the word "a" or "an" when used in conjunction
with the term "comprising" in the claims and/or the specification
may mean "one," but it is also consistent with the meaning of "one
or more," "at least one," and "one or more than one."
[0041] As used in this specification and claim(s), the words
"comprising" (and any form of comprising, such as "comprise" and
"comprises"), "having" (and any form of having, such as "have" and
"has"), "including" (and any form of including, such as "includes"
and "include") or "containing" (and any form of containing, such as
"contains" and "contain") are inclusive or open-ended and do not
exclude additional, unrecited elements or method steps.
[0042] The compositions and methods for their use can "comprise,"
"consist essentially of," or "consist of" any of the ingredients or
steps disclosed throughout the specification.
[0043] Other objects, features and advantages of the present
invention will become apparent from the following detailed
description. It should be understood, however, that the detailed
description and the examples, while indicating specific embodiments
of the invention, are given by way of illustration only.
Additionally, it is contemplated that changes and modifications
within the spirit and scope of the invention will become apparent
to those skilled in the art from this detailed description.
DESCRIPTION OF ILLUSTRATIVE EMBODIMENTS
[0044] As noted above, several of the unique aspects of the present
invention are the combination of hydrolyzed algin, zinc sulfate,
and saccharide isomerate in a topical composition and the use of
such composition to moisturize and/or improve the appearance and/or
condition of skin and/or hair, increase filaggrin production,
increase skin moisture, increase occludin production, inhibit
TNF.alpha. production, prevent oxidative damage, inhibit
PPAR-.gamma. activity, inhibit MMP1 activity, inhibit MMP9
activity, and/or inhibit elastase activity. This allows for the
benefits of stable topical compositions with the benefits
outlined.
[0045] Some embodiments are designed to work as a moisturizer. An
example of such a composition is provided in Example 1, Table 1.
Some embodiments are designed to work as a mask. An example of such
a composition is provided in Example 1, Table 2. Some embodiments
are designed to work as a foundation. An example of such a
composition is provided in Example 1, Table 3. Some embodiments are
designed to work as a freshener. An example of such a composition
is provided in Example 1, Table 4. Some embodiments are designed to
work as a cleanser. An example of such a composition is provided in
Example 1, Tables 5, 6, 7, and 8.
[0046] These and other non-limiting aspects of the present
invention are provided in the following subsections.
A. Determining Skin-Type
[0047] The compositions of the present invention utilize unique
combinations of ingredients, which can be used to create a
formulation for a particular skin type (e.g., normal, dry, oily, or
combination skin). The compositions of the present invention,
however, can be used across all skin types while reducing any skin
irritating effects. For instance, the unique combination of
ingredients disclosed herein can be used for, but is not limited to
use for, oily skin and/or hair.
[0048] The following are non-limiting examples of how skin type may
be determined. There are also other well-known methods for
determining a person's skin type. There are three main skin types:
(1) normal skin; (2) dry skin; and (3) oily skin. A fourth skin
type is simply a combination of any one of normal, dry, or oily
skin (e.g., normal/dry, normal/oily, oily/dry).
[0049] Normal skin, for instance, can be identified as having a
smooth texture and no greasy patches or flaky areas. Therefore, a
product that can retain skin moisture in its present form can be
used to maintain the appearance of normal skin.
[0050] As for dry skin, it has a low level of sebum production from
sebaceous glands and is prone to irritation or erythema. The
appearance of dry skin has a parched look caused by the skin's
inability to retain moisture. Oftentimes it feels "tight" and
uncomfortable after washing and is prone to chapping, flaking, and
cracking. Dry skin can be exacerbated by wind, extremes of
temperature and air-conditioning, all of which cause the skin to
flake, chap and feel tight. Dry skin typically has a dull
appearance. Therefore, a product that deliver appropriate hydration
and restore moisture to dry skin can be used to counteract the
effects of dry skin.
[0051] With respect to oily skin, such skin is shiny, thick and
dull colored. It feels oily and has coarse pores and pimples and
other unsightly blemishes due to overproduction of sebum from
sebaceous glands and from clogged/blocked pores. In this regard,
oily skin usually has oil producing sebaceous glands that are
overactive and produce more oil than is needed. The oil oozes and
gives the skin a greasy shine. The pores are enlarged and the skin
has a coarse look. Therefore, a product that can help control skin
surface oiliness while also retaining appropriate skin moisture can
be used to counteract the effects of oily skin.
[0052] As noted above, combination skin is a combination of both
oily, dry, and/or normal skin (e.g., normal/dry, oily/dry,
normal/oily). For oily/dry skin, there is typically a greasy center
panel consisting of nose, forehead and chin (also known as the
"T-zone" of a person's face) and a dry panel consisting of cheeks,
mouth and the areas around the eyes. Therefore, a product that can
control the excess oil production in sebaceous glands in the T-zone
while also hydrating the dry skin areas outside of the T-zone can
be used for such oily/dry skin.
[0053] Once a particular skin-type is identified, a person can then
select an appropriate composition to correct or maintain the
skin-type.
B. Combination of Ingredients
[0054] It has been found that a combination of
ingredients--hydrolyzed algin, zinc sulfate, and saccharide
isomerate--can be used to moisturize and/or improve the appearance
and/or condition of skin and/or hair. In some embodiments, the
combination of ingredients can be used to moisturize and/or improve
the appearance and/or condition of oily skin and/or hair These
ingredients are discussed in more detail below.
[0055] Saccharide isomerate is an exopolysaccharide synthesized by
a micro-organism called Vibrio alginolyticus and belonging to the
family of Thalasso plankton. In some embodiments this ingredient is
commercially available, e.g., from Barnet (New Jersey, USA), which
provides saccharide isomerate under the trade name Benoiderm. It
has been determined that this ingredient can be used to increase
production of filaggrin, increase skin moisture, increase
production of occludin, inhibit TNF.alpha. production, and prevent
oxidative damage.
[0056] The combination of hydrolyzed algin and zinc sulfate is also
used in the compositions disclosed herein. Hydrolyzed algin is an
anionic polysaccharide produced by Laminaria digitata. In some
instances, the hydrolyzed algin is made at least in party by
enzymatically hydrolyzing alginate. In some instances, alginate is
acid hydrolyzed in pH adjusted water. In some instances, alginate
is enzymatically hydrolyzed and acid hydrolyzed. Zinc sulfate has
the inorganic formula ZnSO.sub.4. Zinc sulfate is also known as
zinc sulphate and white vitriol. These ingredients are commercially
available, e.g., from Barnet under the trade name Phyko ACP. It has
been determined that these combined ingredients can be used to
inhibit PPAR-.gamma. activity, inhibit MMP1 activity, inhibit MMP9
activity, and inhibit elastase activity.
C. Amounts of Ingredients
[0057] It is contemplated that the compositions of the present
invention can include any amount of the ingredients discussed in
this specification. The compositions can also include any number of
combinations of additional ingredients described throughout this
specification (e.g., pigments, or additional cosmetic or
pharmaceutical ingredients). The concentrations of the any
ingredient within the compositions can vary. In non-limiting
embodiments, for example, the compositions can comprise, consisting
essentially of, or consist of, in their final form, for example, at
least about 0.0001%, 0.0002%, 0.0003%, 0.0004%, 0.0005%, 0.0006%,
0.0007%, 0.0008%, 0.0009%, 0.0010%, 0.0011%, 0.0012%, 0.0013%,
0.0014%, 0.0015%, 0.0016%, 0.0017%, 0.0018%, 0.0019%, 0.0020%,
0.0021%, 0.0022%, 0.0023%, 0.0024%, 0.0025%, 0.0026%, 0.0027%,
0.0028%, 0.0029%, 0.0030%, 0.0031%, 0.0032%, 0.0033%, 0.0034%,
0.0035%, 0.0036%, 0.0037%, 0.0038%, 0.0039%, 0.0040%, 0.0041%,
0.0042%, 0.0043%, 0.0044%, 0.0045%, 0.0046%, 0.0047%, 0.0048%,
0.0049%, 0.0050%, 0.0051%, 0.0052%, 0.0053%, 0.0054%, 0.0055%,
0.0056%, 0.0057%, 0.0058%, 0.0059%, 0.0060%, 0.0061%, 0.0062%,
0.0063%, 0.0064%, 0.0065%, 0.0066%, 0.0067%, 0.0068%, 0.0069%,
0.0070%, 0.0071%, 0.0072%, 0.0073%, 0.0074%, 0.0075%, 0.0076%,
0.0077%, 0.0078%, 0.0079%, 0.0080%, 0.0081%, 0.0082%, 0.0083%,
0.0084%, 0.0085%, 0.0086%, 0.0087%, 0.0088%, 0.0089%, 0.0090%,
0.0091%, 0.0092%, 0.0093%, 0.0094%, 0.0095%, 0.0096%, 0.0097%,
0.0098%, 0.0099%, 0.0100%, 0.0200%, 0.0250%, 0.0275%, 0.0300%,
0.0325%, 0.0350%, 0.0375%, 0.0400%, 0.0425%, 0.0450%, 0.0475%,
0.0500%, 0.0525%, 0.0550%, 0.0575%, 0.0600%, 0.0625%, 0.0650%,
0.0675%, 0.0700%, 0.0725%, 0.0750%, 0.0775%, 0.0800%, 0.0825%,
0.0850%, 0.0875%, 0.0900%, 0.0925%, 0.0950%, 0.0975%, 0.1000%,
0.1250%, 0.1500%, 0.1750%, 0.2000%, 0.2250%, 0.2500%, 0.2750%,
0.3000%, 0.3250%, 0.3500%, 0.3750%, 0.4000%, 0.4250%, 0.4500%,
0.4750%, 0.5000%, 0.5250%, 0.0550%, 0.5750%, 0.6000%, 0.6250%,
0.6500%, 0.6750%, 0.7000%, 0.7250%, 0.7500%, 0.7750%, 0.8000%,
0.8250%, 0.8500%, 0.8750%, 0.9000%, 0.9250%, 0.9500%, 0.9750%,
1.0%, 1.1%, 1.2%, 1.3%, 1.4%, 1.5%, 1.6%, 1.7%, 1.8%, 1.9%, 2.0%,
2.1%, 2.2%, 2.3%, 2.4%, 2.5%, 2.6%, 2.7%, 2.8%, 2.9%, 3.0%, 3.1%,
3.2%, 3.3%, 3.4%, 3.5%, 3.6%, 3.7%, 3.8%, 3.9%, 4.0%, 4.1%, 4.2%,
4.3%, 4.4%, 4.5%, 4.6%, 4.7%, 4.8%, 4.9%, 5.0%, 5.1%, 5.2%, 5.3%,
5.4%, 5.5%, 5.6%, 5.7%, 5.8%, 5.9%, 6.0%, 6.1%, 6.2%, 6.3%, 6.4%,
6.5%, 6.6%, 6.7%, 6.8%, 6.9%, 7.0%, 7.1%, 7.2%, 7.3%, 7.4%, 7.5%,
7.6%, 7.7%, 7.8%, 7.9%, 8.0%, 8.1%, 8.2%, 8.3%, 8.4%, 8.5%, 8.6%,
8.7%, 8.8%, 8.9%, 9.0%, 9.1%, 9.2%, 9.3%, 9.4%, 9.5%, 9.6%, 9.7%,
9.8%, 9.9%, 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20%,
21%, 22%, 23%, 24%, 25%, 26%, 27%, 28%, 29%, 30%, 35%, 40%, 45%,
50%, 60%, 65%, 70%, 75%, 80%, 85%, 90%, 95%, or 99% or any range
derivable therein, of at least one of the ingredients that are
mentioned throughout the specification and claims. In non-limiting
aspects, the percentage can be calculated by weight or volume of
the total composition. A person of ordinary skill in the art would
understand that the concentrations can vary depending on the
addition, substitution, and/or subtraction of ingredients in a
given composition.
D. Vehicles
[0058] The compositions of the present invention can include or be
incorporated into all types of vehicles and carriers. The vehicle
or carrier can be a pharmaceutically or dermatologically acceptable
vehicle or carrier. Non-limiting examples of vehicles or carriers
include water, glycerin, alcohol, oil, a silicon containing
compound, a silicone compound, and wax. Variations and other
appropriate vehicles will be apparent to the skilled artisan and
are appropriate for use in the present invention. In certain
aspects, the concentrations and combinations of the compounds,
ingredients, and agents can be selected in such a way that the
combinations are chemically compatible and do not form complexes
which precipitate from the finished product.
E. Structure
[0059] The compositions of the present invention can be structured
or formulated into a variety of different forms. Non-limiting
examples include emulsions (e.g., water-in-oil,
water-in-oil-in-water, oil-in-water, silicone-in-water,
water-in-silicone, oil-in-water-in-oil, oil-in-water-in-silicone
emulsions), creams, lotions, solutions (both aqueous and
hydro-alcoholic), anhydrous bases (such as lipsticks and powders),
gels, masks, peels, and ointments. Variations and other structures
will be apparent to the skilled artisan and are appropriate for use
in the present invention.
F. Additional Ingredients
[0060] In addition to the combination of ingredients disclosed by
the inventors, the compositions can also include additional
ingredients such as cosmetic ingredients and pharmaceutical active
ingredients. Non-limiting examples of these additional ingredients
are described in the following subsections.
[0061] 1. Cosmetic Ingredients
[0062] The CTFA International Cosmetic Ingredient Dictionary and
Handbook (2004 and 2008) describes a wide variety of non-limiting
cosmetic ingredients that can be used in the context of the present
invention. Examples of these ingredient classes include: fragrance
agents (artificial and natural; e.g., gluconic acid,
phenoxyethanol, and triethanolamine), dyes and color ingredients
(e.g., Blue 1, Blue 1 Lake, Red 40, titanium dioxide, D&C blue
no. 4, D&C green no. 5, D&C orange no. 4, D&C red no.
17, D&C red no. 33, D&C violet no. 2, D&C yellow no.
10, and D&C yellow no. 11), flavoring agents/aroma agents
(e.g., Stevia rebaudiana (sweetleaf) extract, and menthol),
adsorbents, lubricants, solvents, moisturizers (including, e.g.,
emollients, humectants, film formers, occlusive agents, and agents
that affect the natural moisturization mechanisms of the skin),
water-repellants, UV absorbers (physical and chemical absorbers
such as para-aminobenzoic acid ("PABA") and corresponding PABA
derivatives, titanium dioxide, zinc oxide, etc.), essential oils,
vitamins (e.g., A, B, C, D, E, and K), trace metals (e.g., zinc,
calcium and selenium), anti-irritants (e.g., steroids and
non-steroidal anti-inflammatories), botanical extracts (e.g., Aloe
vera, chamomile, cucumber extract, Ginkgo biloba, ginseng, and
rosemary), anti-microbial agents, antioxidants (e.g., BHT and
tocopherol), chelating agents (e.g., disodium EDTA and tetrasodium
EDTA), preservatives (e.g., methylparaben and propylparaben), pH
adjusters (e.g., sodium hydroxide and citric acid), absorbents
(e.g., aluminum starch octenylsuccinate, kaolin, corn starch, oat
starch, cyclodextrin, talc, and zeolite), skin bleaching and
lightening agents (e.g., hydroquinone and niacinamide lactate),
humectants (e.g., sorbitol, urea, methyl gluceth-20, plankton
extract, and mannitol), exfoliants, waterproofing agents (e.g.,
magnesium/aluminum hydroxide stearate), skin conditioning agents
(e.g., aloe extracts, allantoin, bisabolol, ceramides, dimethicone,
hyaluronic acid, biosaccharide gum-1, ethylhexylglycerin, pentylene
glycol, hydrogenated polydecene, octyldodecyl oleate, and
dipotassium glycyrrhizate). Non-limiting examples of some of these
ingredients are provided in the following subsections.
[0063] The extracts described herein can be extracts made through
extraction methods known in the art and combinations thereof.
Non-limiting examples of extraction methods include the use of
liquid-liquid extraction, solid phase extraction, aqueous
extraction, ethyl acetate, alcohol, acetone, oil, supercritical
carbon dioxide, heat, pressure, pressure drop extraction,
ultrasonic extraction, etc. Extracts can be a liquid, solid, dried
liquid, re-suspended solid, etc.
[0064] a. UV Absorption Agents
[0065] UV absorption agents that can be used in combination with
the compositions of the present invention include chemical and
physical sunblocks. Non-limiting examples of chemical sunblocks
that can be used include para-aminobenzoic acid (PABA), PABA esters
(glyceryl PABA, amyldimethyl PABA and octyldimethyl PABA), butyl
PABA, ethyl PABA, ethyl dihydroxypropyl PABA, benzophenones
(oxybenzone, sulisobenzone, benzophenone, and benzophenone-1
through 12), cinnamates (octyl methoxycinnamate, isoamyl
p-methoxycinnamate, octylmethoxy cinnamate, cinoxate, diisopropyl
methyl cinnamate, DEA-methoxycinnamate, ethyl diisopropylcinnamate,
glyceryl octanoate dimethoxycinnamate and ethyl methoxycinnamate),
cinnamate esters, salicylates (homomethyl salicylate, benzyl
salicylate, glycol salicylate, isopropylbenzyl salicylate, etc.),
anthranilates, ethyl urocanate, homosalate, octisalate,
dibenzoylmethane derivatives (e.g., avobenzone), octocrylene, octyl
triazone, digalloyl trioleate, glyceryl aminobenzoate, lawsone with
dihydroxyacetone, ethylhexyl triazone, dioctyl butamido triazone,
benzylidene malonate polysiloxane, terephthalylidene dicamphor
sulfonic acid, disodium phenyl dibenzimidazole tetrasulfonate,
diethylamino hydroxybenzoyl hexyl benzoate, bis diethylamino
hydroxybenzoyl benzoate, bis benzoxazoylphenyl ethylhexylimino
triazine, drometrizole trisiloxane, methylene bis-benzotriazolyl
tetramethylbutylphenol, and bis-ethylhexyloxyphenol
methoxyphenyltriazine, 4-methylbenzylidene camphor, and isopentyl
4-methoxycinnamate. Non-limiting examples of physical sunblocks
include, kaolin, talc, petrolatum and metal oxides (e.g., titanium
dioxide and zinc oxide).
[0066] b. Moisturizing Agents
[0067] Non-limiting examples of moisturizing agents that can be
used with the compositions of the present invention include amino
acids, chondroitin sulfate, diglycerin, erythritol, fructose,
glucose, glycerin, glycerol polymers, glycol, 1,2,6-hexanetriol,
honey, hyaluronic acid, hydrogenated honey, hydrogenated starch
hydrolysate, inositol, lactitol, maltitol, maltose, mannitol,
natural moisturizing factor, PEG-15 butanediol, plankton extract,
polyglyceryl sorbitol, salts of pyrrolidone carboxylic acid,
potassium PCA, propylene glycol, sodium glucuronate, sodium PCA,
sorbitol, sucrose, trehalose, urea, and xylitol.
[0068] Other examples include acetylated lanolin, acetylated
lanolin alcohol, alanine, algae extract, Aloe barbadensis, Aloe
barbadensis extract, Aloe barbadensis gel, Althea officinalis
extract, apricot (Prunus armeniaca) kernel oil, arginine, arginine
aspartate, Arnica montana extract, aspartic acid, avocado (Persea
gratissima) oil, barrier sphingolipids, butyl alcohol, beeswax,
behenyl alcohol, beta-sitosterol, birch (Betula alba) bark extract,
borage (Borago officinalis) extract, butcherbroom (Ruscus
aculeatus) extract, butylene glycol, Calendula officinalis extract,
Calendula officinalis oil, candelilla (Euphorbia cerifera) wax,
canola oil, caprylic/capric triglyceride, cardamom (Elettaria
cardamomum) oil, carnauba (Copernicia cerifera) wax, carrot (Daucus
carota sativa) oil, castor (Ricinus communis) oil, ceramides,
ceresin, ceteareth-5, ceteareth-12, ceteareth-20, cetearyl
octanoate, ceteth-20, ceteth-24, cetyl acetate, cetyl octanoate,
cetyl palmitate, chamomile (Anthemis nobilis) oil, cholesterol,
cholesterol esters, cholesteryl hydroxystearate, citric acid, clary
(Salvia sclarea) oil, cocoa (Theobroma cacao) butter,
coco-caprylate/caprate, coconut (Cocos nucifera) oil, collagen,
collagen amino acids, corn (Zea mays) oil, fatty acids, decyl
oleate, dimethicone copolyol, dimethiconol, dioctyl adipate,
dioctyl succinate, dipentaerythrityl hexacaprylate/hexacaprate,
DNA, erythritol, ethoxydiglycol, ethyl linoleate, Eucalyptus
globulus oil, evening primrose (Oenothera biennis) oil, fatty
acids, Geranium maculatum oil, glucosamine, glucose glutamate,
glutamic acid, glycereth-26, glycerin, glycerol, glyceryl
distearate, glyceryl hydroxystearate, glyceryl laurate, glyceryl
linoleate, glyceryl myristate, glyceryl oleate, glyceryl stearate,
glyceryl stearate SE, glycine, glycol stearate, glycol stearate SE,
glycosaminoglycans, grape (Vitis vinifera) seed oil, hazel (Corylus
americana) nut oil, hazel (Corylus avellana) nut oil, hexylene
glycol, hyaluronic acid, hybrid safflower (Carthamus tinctorius)
oil, hydrogenated castor oil, hydrogenated coco-glycerides,
hydrogenated coconut oil, hydrogenated lanolin, hydrogenated
lecithin, hydrogenated palm glyceride, hydrogenated palm kernel
oil, hydrogenated soybean oil, hydrogenated tallow glyceride,
hydrogenated vegetable oil, hydrolyzed collagen, hydrolyzed
elastin, hydrolyzed glycosaminoglycans, hydrolyzed keratin,
hydrolyzed soy protein, hydroxylated lanolin, hydroxyproline,
isocetyl stearate, isocetyl stearoyl stearate, isodecyl oleate,
isopropyl isostearate, isopropyl lanolate, isopropyl myristate,
isopropyl palmitate, isopropyl stearate, isostearamide DEA,
isostearic acid, isostearyl lactate, isostearyl neopentanoate,
jasmine (Jasminum officinale) oil, jojoba (Buxus chinensis) oil,
kelp, kukui (Aleurites moluccana) nut oil, lactamide MEA,
laneth-16, laneth-10 acetate, lanolin, lanolin acid, lanolin
alcohol, lanolin oil, lanolin wax, lavender (Lavandula
angustifolia) oil, lecithin, lemon (Citrus medica limonum) oil,
linoleic acid, linolenic acid, Macadamia ternifolia nut oil,
maltitol, matricaria (Chamomilla recutita) oil, methyl glucose
sesquistearate, methylsilanol PCA, mineral oil, mink oil,
mortierella oil, myristyl lactate, myristyl myristate, myristyl
propionate, neopentyl glycol dicaprylate/dicaprate, octyldodecanol,
octyldodecyl myristate, octyldodecyl stearoyl stearate, octyl
hydroxystearate, octyl palmitate, octyl salicylate, octyl stearate,
oleic acid, olive (Olea europaea) oil, orange (Citrus aurantium
dulcis) oil, palm (Elaeis guineensis) oil, palmitic acid,
pantethine, panthenol, panthenyl ethyl ether, paraffin, PCA, peach
(Prunus persica) kernel oil, peanut (Arachis hypogaea) oil, PEG-8
C12-18 ester, PEG-15 cocamine, PEG-150 distearate, PEG-60 glyceryl
isostearate, PEG-5 glyceryl stearate, PEG-30 glyceryl stearate,
PEG-7 hydrogenated castor oil, PEG-40 hydrogenated castor oil,
PEG-60 hydrogenated castor oil, PEG-20 methyl glucose
sesquistearate, PEG-40 sorbitan peroleate, PEG-5 soy sterol, PEG-10
soy sterol, PEG-2 stearate, PEG-8 stearate, PEG-20 stearate, PEG-32
stearate, PEG-40 stearate, PEG-50 stearate, PEG-100 stearate,
PEG-150 stearate, pentadecalactone, peppermint (Mentha piperita)
oil, petrolatum, phospholipids, plankton extract, polyamino sugar
condensate, polyglyceryl-3 diisostearate, polyquaternium-24,
polysorbate 20, polysorbate 40, polysorbate 60, polysorbate 80,
polysorbate 85, potassium myristate, potassium palmitate, propylene
glycol, propylene glycol dicaprylate/dicaprate, propylene glycol
dioctanoate, propylene glycol dipelargonate, propylene glycol
laurate, propylene glycol stearate, propylene glycol stearate SE,
PVP, pyridoxine dipalmitate, retinol, retinyl palmitate, rice
(Oryza sativa) bran oil, RNA, rosemary (Rosmarinus officinalis)
oil, rose oil, safflower (Carthamus tinctorius) oil, sage (Salvia
officinalis) oil, sandalwood (Santalum album) oil, serine, serum
protein, sesame (Sesamum indicum) oil, shea butter (Butyrospermum
parkii), silk powder, sodium chondroitin sulfate, sodium
hyaluronate, sodium lactate, sodium palmitate, sodium PCA, sodium
polyglutamate, soluble collagen, sorbitan laurate, sorbitan oleate,
sorbitan palmitate, sorbitan sesquioleate, sorbitan stearate,
sorbitol, soybean (Glycine soja) oil, sphingolipids, squalane,
squalene, stearamide MEA-stearate, stearic acid, stearoxy
dimethicone, stearoxytrimethylsilane, stearyl alcohol, stearyl
glycyrrhetinate, stearyl heptanoate, stearyl stearate, sunflower
(Helianthus annuus) seed oil, sweet almond (Prunus amygdalus
dulcis) oil, synthetic beeswax, tocopherol, tocopheryl acetate,
tocopheryl linoleate, tribehenin, tridecyl neopentanoate, tridecyl
stearate, triethanolamine, tristearin, urea, vegetable oil, water,
waxes, wheat (Triticum vulgare) germ oil, and ylang ylang (Cananga
odorata) oil.
[0069] c. Antioxidants
[0070] Non-limiting examples of antioxidants that can be used with
the compositions of the present invention include acetyl cysteine,
ascorbic acid polypeptide, ascorbyl dipalmitate, ascorbyl
methylsilanol pectinate, ascorbyl palmitate, ascorbyl stearate,
BHA, BHT, t-butyl hydroquinone, cysteine, cysteine HCI,
diamylhydroquinone, di-t-butylhydroquinone, dicetyl
thiodipropionate, dioleyl tocopheryl methylsilanol, disodium
ascorbyl sulfate, distearyl thiodipropionate, ditridecyl
thiodipropionate, dodecyl gallate, erythorbic acid, esters of
ascorbic acid, ethyl ferulate, ferulic acid, gallic acid esters,
hydroquinone, isooctyl thioglycolate, kojic acid, magnesium
ascorbate, magnesium ascorbyl phosphate, methylsilanol ascorbate,
natural botanical anti-oxidants such as green tea or grape seed
extracts, nordihydroguaiaretic acid, octyl gallate,
phenylthioglycolic acid, potassium ascorbyl tocopheryl phosphate,
potassium sulfite, propyl gallate, quinones, rosmarinic acid,
sodium ascorbate, sodium bisulfite, sodium erythorbate, sodium
metabisulfite, sodium sulfite, superoxide dismutase, sodium
thioglycolate, sorbityl furfural, thiodiglycol, thiodiglycolamide,
thiodiglycolic acid, thioglycolic acid, thiolactic acid,
thiosalicylic acid, tocophereth-5, tocophereth-10, tocophereth-12,
tocophereth-18, tocophereth-50, tocopherol, tocophersolan,
tocopheryl acetate, tocopheryl linoleate, tocopheryl nicotinate,
tocopheryl succinate, and tris(nonylphenyl)phosphite.
[0071] d. Structuring Agents
[0072] In other non-limiting aspects, the compositions of the
present invention can include a structuring agent. Structuring
agent, in certain aspects, assist in providing rheological
characteristics to the composition to contribute to the
composition's stability. In other aspects, structuring agents can
also function as an emulsifier or surfactant. Non-limiting examples
of structuring agents include stearic acid, palmitic acid, stearyl
alcohol, cetyl alcohol, behenyl alcohol, stearic acid, palmitic
acid, the polyethylene glycol ether of stearyl alcohol having an
average of about 1 to about 21 ethylene oxide units, the
polyethylene glycol ether of cetyl alcohol having an average of
about 1 to about 5 ethylene oxide units, and mixtures thereof.
[0073] e. Emulsifiers
[0074] In certain aspects of the present invention, the
compositions do not include an emulsifier. In other aspects,
however, the compositions can include one or more emulsifiers.
Emulsifiers can reduce the interfacial tension between phases and
improve the formulation and stability of an emulsion. The
emulsifiers can be nonionic, cationic, anionic, and zwitterionic
emulsifiers (See McCutcheon's (1986); U.S. Pat. Nos. 5,011,681;
4,421,769; 3,755,560). Non-limiting examples include esters of
glycerin, esters of propylene glycol, fatty acid esters of
polyethylene glycol, fatty acid esters of polypropylene glycol,
esters of sorbitol, esters of sorbitan anhydrides, carboxylic acid
copolymers, esters and ethers of glucose, ethoxylated ethers,
ethoxylated alcohols, alkyl phosphates, polyoxyethylene fatty ether
phosphates, fatty acid amides, acyl lactylates, soaps, TEA
stearate, DEA oleth-3 phosphate, polyethylene glycol 20 sorbitan
monolaurate (polysorbate 20), polyethylene glycol 5 soya sterol,
steareth-2, steareth-20, steareth-21, ceteareth-20, cetearyl
glucoside, cetearyl alcohol, C12-13 pareth-3, PPG-2 methyl glucose
ether distearate, PPG-5-ceteth-20, bis-PEG/PPG-20/20 dimethicone,
ceteth-10, polysorbate 80, cetyl phosphate, potassium cetyl
phosphate, diethanolamine cetyl phosphate, polysorbate 60, glyceryl
stearate, PEG-100 stearate, arachidyl alcohol, arachidyl glucoside,
and mixtures thereof.
[0075] f. Silicone Containing Compounds
[0076] In non-limiting aspects, silicone containing compounds
include any member of a family of polymeric products whose
molecular backbone is made up of alternating silicon and oxygen
atoms with side groups attached to the silicon atoms. By varying
the --Si--O-- chain lengths, side groups, and crosslinking,
silicones can be synthesized into a wide variety of materials. They
can vary in consistency from liquid to gel to solids.
[0077] The silicone containing compounds that can be used in the
context of the present invention include those described in this
specification or those known to a person of ordinary skill in the
art. Non-limiting examples include silicone oils (e.g., volatile
and non-volatile oils), gels, and solids. In certain aspects, the
silicon containing compounds includes a silicone oils such as a
polyorganosiloxane. Non-limiting examples of polyorganosiloxanes
include dimethicone, cyclomethicone, poly silicone-11, phenyl
trimethicone, trimethylsilylamodimethicone,
stearoxytrimethylsilane, or mixtures of these and other
organosiloxane materials in any given ratio in order to achieve the
desired consistency and application characteristics depending upon
the intended application (e.g., to a particular area such as the
skin, hair, or eyes). A "volatile silicone oil" includes a silicone
oil have a low heat of vaporization, i.e. normally less than about
50 cal per gram of silicone oil. Non-limiting examples of volatile
silicone oils include: cyclomethicones such as Dow Corning 344
Fluid, Dow Corning 345 Fluid, Dow Corning 244 Fluid, and Dow
Corning 245 Fluid, Volatile Silicon 7207 (Union Carbide Corp.,
Danbury, Conn.); low viscosity dimethicones, i.e. dimethicones
having a viscosity of about 50 cst or less (e.g., dimethicones such
as Dow Corning 200-0.5 cst Fluid). The Dow Corning Fluids are
available from Dow Corning Corporation, Midland, Mich.
Cyclomethicone and dimethicone are described in the Third Edition
of the CTFA Cosmetic Ingredient Dictionary (incorporated by
reference) as cyclic dimethyl polysiloxane compounds and a mixture
of fully methylated linear siloxane polymers end-blocked with
trimethylsiloxy units, respectively. Other non-limiting volatile
silicone oils that can be used in the context of the present
invention include those available from General Electric Co.,
Silicone Products Div., Waterford, N.Y. and SWS Silicones Div. of
Stauffer Chemical Co., Adrian, Michigan.
[0078] g. Essential Oils
[0079] Essential oils include oils derived from herbs, flowers,
trees, and other plants. Such oils are typically present as tiny
droplets between the plant's cells, and can be extracted by several
method known to those of skill in the art (e.g., steam distilled,
enfleurage (i.e., extraction by using fat), maceration, solvent
extraction, or mechanical pressing). When these types of oils are
exposed to air they tend to evaporate (i.e., a volatile oil). As a
result, many essential oils are colorless, but with age they can
oxidize and become darker. Essential oils are insoluble in water
and are soluble in alcohol, ether, fixed oils (vegetal), and other
organic solvents. Typical physical characteristics found in
essential oils include boiling points that vary from about
160.degree. to 240.degree. C. and densities ranging from about
0.759 to about 1.096.
[0080] Essential oils typically are named by the plant from which
the oil is found. For example, rose oil or peppermint oil are
derived from rose or peppermint plants, respectively. Non-limiting
examples of essential oils that can be used in the context of the
present invention include sesame oil, macadamia nut oil, tea tree
oil, evening primrose oil, Spanish sage oil, Spanish rosemary oil,
coriander oil, thyme oil, pimento berries oil, rose oil, anise oil,
balsam oil, bergamot oil, rosewood oil, cedar oil, chamomile oil,
sage oil, clary sage oil, clove oil, cypress oil, eucalyptus oil,
fennel oil, sea fennel oil, frankincense oil, geranium oil, ginger
oil, grapefruit oil, jasmine oil, juniper oil, lavender oil, lemon
oil, lemongrass oil, lime oil, mandarin oil, marjoram oil, myrrh
oil, neroli oil, orange oil, patchouli oil, pepper oil, black
pepper oil, petitgrain oil, pine oil, rose otto oil, rosemary oil,
sandalwood oil, spearmint oil, spikenard oil, vetiver oil,
wintergreen oil, or ylang ylang. Other essential oils known to
those of skill in the art are also contemplated as being useful
within the context of the present invention.
[0081] h. Thickening Agents
[0082] Thickening agents, including thickener or gelling agents,
include substances which that can increase the viscosity of a
composition. Thickeners includes those that can increase the
viscosity of a composition without substantially modifying the
efficacy of the active ingredient within the composition.
Thickeners can also increase the stability of the compositions of
the present invention. In certain aspects of the present invention,
thickeners include hydrogenated polyisobutene, trihydroxystearin,
ammonium acryloyldimethyltaurate/vp copolymer, or a mixture of
them.
[0083] Non-limiting examples of additional thickening agents that
can be used in the context of the present invention include
carboxylic acid polymers, crosslinked polyacrylate polymers,
polyacrylamide polymers, polysaccharides, and gums. Examples of
carboxylic acid polymers include crosslinked compounds containing
one or more monomers derived from acrylic acid, substituted acrylic
acids, and salts and esters of these acrylic acids and the
substituted acrylic acids, wherein the crosslinking agent contains
two or more carbon-carbon double bonds and is derived from a
polyhydric alcohol (see U.S. Pat. Nos. 5,087,445; 4,509,949;
2,798,053; CTFA International Cosmetic Ingredient Dictionary,
Fourth edition, 1991, pp. 12 and 80). Examples of commercially
available carboxylic acid polymers include carbomers, which are
homopolymers of acrylic acid crosslinked with allyl ethers of
sucrose or pentaerytritol (e.g., Carbopol.TM. 900 series from B. F.
Goodrich).
[0084] Non-limiting examples of crosslinked polyacrylate polymers
include cationic and nonionic polymers. Examples are described in
U.S. Pat. Nos. 5,100,660; 4,849,484; 4,835,206; 4,628,078;
4,599,379).
[0085] Non-limiting examples of polyacrylamide polymers (including
nonionic polyacrylamide polymers including substituted branched or
unbranched polymers) include polyacrylamide, isoparaffin and
laureth-7, multi-block copolymers of acrylamides and substituted
acrylamides with acrylic acids and substituted acrylic acids.
[0086] Non-limiting examples of polysaccharides include cellulose,
carboxymethyl hydroxyethylcellulose, cellulose acetate propionate
carboxylate, hydroxyethylcellulose, hydroxyethyl ethylcellulose,
hydroxypropylcellulose, hydroxypropyl methylcellulose, methyl
hydroxyethylcellulose, microcrystalline cellulose, sodium cellulose
sulfate, and mixtures thereof. Another example is an alkyl
substituted cellulose where the hydroxy groups of the cellulose
polymer is hydroxyalkylated (preferably hydroxy ethylated or
hydroxypropylated) to form a hydroxyalkylated cellulose which is
then further modified with a C10-C30 straight chain or branched
chain alkyl group through an ether linkage. Typically these
polymers are ethers of C10-C30 straight or branched chain alcohols
with hydroxyalkylcelluloses. Other useful polysaccharides include
scleroglucans comprising a linear chain of (1-3) linked glucose
units with a (1-6) linked glucose every three unit.
[0087] Non-limiting examples of gums that can be used with the
present invention include acacia, agar, algin, alginic acid,
ammonium alginate, amylopectin, calcium alginate, calcium
carrageenan, carnitine, carrageenan, dextrin, gelatin, gellan gum,
guar gum, guar hydroxypropyltrimonium chloride, hectorite,
hyaluronic acid, hydrated silica, hydroxypropyl chitosan,
hydroxypropyl guar, karaya gum, kelp, locust bean gum, natto gum,
potassium alginate, potassium carrageenan, propylene glycol
alginate, sclerotium gum, sodium carboxymethyl dextran, sodium
carrageenan, tragacanth gum, xanthan gum, and mixtures thereof.
[0088] i. Preservatives
[0089] Non-limiting examples of preservatives that can be used in
the context of the present invention include quaternary ammonium
preservatives such as polyquaternium-1 and benzalkonium halides
(e.g., benzalkonium chloride ("BAC") and benzalkonium bromide),
parabens (e.g., methylparabens and propylparabens), phenoxyethanol,
benzyl alcohol, chlorobutanol, phenol, sorbic acid, thimerosal or
combinations thereof.
[0090] 2. Pharmaceutical Ingredients
[0091] Pharmaceutical active agents are also contemplated as being
useful with the compositions of the present invention. Non-limiting
examples of pharmaceutical active agents include anti-acne agents,
agents used to treat rosacea, analgesics, anesthetics, anorectals,
antihistamines, anti-inflammatory agents including non-steroidal
anti-inflammatory drugs, antibiotics, antifungals, antivirals,
antimicrobials, anti-cancer actives, scabicides, pediculicides,
antineoplastics, antiperspirants, antipruritics, antipsoriatic
agents, antiseborrheic agents, biologically active proteins and
peptides, burn treatment agents, cauterizing agents, depigmenting
agents, depilatories, diaper rash treatment agents, enzymes, hair
growth stimulants, hair growth retardants including DFMO and its
salts and analogs, hemostatics, kerotolytics, canker sore treatment
agents, cold sore treatment agents, dental and periodontal
treatment agents, photosensitizing actives, skin protectant/barrier
agents, steroids including hormones and corticosteroids, sunburn
treatment agents, sunscreens, transdermal actives, nasal actives,
vaginal actives, wart treatment agents, wound treatment agents,
wound healing agents, etc.
G. Kits
[0092] Kits are also contemplated as being used in certain aspects
of the present invention. For instance, compositions of the present
invention can be included in a kit. A kit can include a container.
Containers can include a bottle, a metal tube, a laminate tube, a
plastic tube, a dispenser, a pressurized container, a barrier
container, a package, a compartment, a lipstick container, a
compact container, cosmetic pans that can hold cosmetic
compositions, or other types of containers such as injection or
blow-molded plastic containers into which the dispersions or
compositions or desired bottles, dispensers, or packages are
retained. The kit and/or container can include indicia on its
surface. The indicia, for example, can be a word, a phrase, an
abbreviation, a picture, or a symbol.
[0093] The containers can dispense a pre-determined amount of the
composition. In other embodiments, the container can be squeezed
(e.g., metal, laminate, or plastic tube) to dispense a desired
amount of the composition. The composition can be dispensed as a
spray, an aerosol, a liquid, a fluid, or a semi-solid. The
containers can have spray, pump, or squeeze mechanisms. A kit can
also include instructions for employing the kit components as well
the use of any other compositions included in the container.
Instructions can include an explanation of how to apply, use, and
maintain the compositions.
EXAMPLES
[0094] The following examples are included to demonstrate preferred
embodiments of the invention. It should be appreciated by those of
skill in the art that the techniques disclosed in the examples
which follow represent techniques discovered by the inventor to
function well in the practice of the invention, and thus can be
considered to constitute preferred modes for its practice. However,
those of skill in the art should, in light of the present
disclosure, appreciate that many changes can be made in the
specific embodiments which are disclosed and still obtain a like or
similar result without departing from the spirit and scope of the
invention.
Example 1
[0095] Formulations having the ingredients from Example 1 were
prepared as topical skin and/or hair compositions. The formulation
in Table 1 was prepared as a moisturizer. The formulation in Table
2 was prepared as a mask. The formulation in Table 3 was prepared
as a foundation. The formulation in Table 4 was prepared as a
freshener. The formulations in Tables 5 to 9 were prepared as
cleansers.
[0096] All of the compositions and/or methods disclosed and claimed
herein can be made and executed without undue experimentation in
light of the present disclosure. While the compositions and methods
of this invention have been described in terms of preferred
embodiments, it will be apparent to those of skill in the art that
variations may be applied to the compositions and/or methods and in
the steps or in the sequence of steps of the method described
herein without departing from the concept, spirit and scope of the
invention. More specifically, it will be apparent that certain
agents which are both chemically and physiologically related may be
substituted for the agents described herein while the same or
similar results would be achieved. All such similar substitutes and
modifications apparent to those skilled in the art are deemed to be
within the spirit, scope and concept of the invention as defined by
the appended claims.
TABLE-US-00001 TABLE 1* Ingredient % Concentration (by weight)
Water 53 Glycerin 25 Cetearyl ethylhexanoate 5 Pentylene glycol 4
Biosaccharide gum-1 3 Dimethicone 3 Silica 2 Cyclopentasiloxane 2
Ammonium acryloyldimethyltaurate/VP 2 copolymer Phenoxyethanol 0.8
PEG-12 dimethicone 0.7 Fragrance (optional) 0.5 Caprylyl glycol 0.3
Chlorphenesin 0.2 Dimethiconol 0.1 Dipotassium glycyrrhizate 0.1
Hydrolyzed algin 0.05 Saccharide isomerate 0.01 Zinc sulfate 0.005
Opuntia tuna fruit extract (optional) 0.0005 Excipients** q.s.
*Formulation can be prepared by mixing the ingredients in a beaker
under heat 70-75.degree. C. until homogenous. Subsequently, the
formulation can be cooled to standing room temperature
(20-25.degree. C.). Further, and if desired, additional ingredients
can be added, for example, to modify the rheological properties of
the composition. **Excipients can be added, for example, to modify
the rheological properties of the composition. Alternatively, the
amount of water can be varied so long as the amount of water in the
composition is at least 40% w/w, and preferably between 45 to 70%
w/w.
TABLE-US-00002 TABLE 2* Ingredient % Concentration (by weight)
Water 42 Kaolin 35 C12-15 alcohols benzoate 5 Propylene glycol 5
Titanium dioxide 5 Magnesium aluminum silicate 2 TEA-lauryl sulfate
2 Xanthan gum 1 Phenoxyethanol 0.9 Hydrolyzed algin 0.05 Saccharide
isomerate 0.01 Zinc sulfate 0.005 Benzyl alcohol (optional) 0.8
Caprylyl alcohol (optional) 0.8 Opuntia tuna fruit extract
(optional) 0.0005 Excipients** q.s. *Formulation can be prepared by
mixing the ingredients in a beaker under heat 70-75.degree. C.
until homogenous. Subsequently, the formulation can be cooled to
standing room temperature (20-25.degree. C.). Further, and if
desired, additional ingredients can be added, for example, to
modify the rheological properties of the composition. **Excipients
can be added, for example, to modify the rheological properties of
the composition. Alternatively, the amount of water can be varied
so long as the amount of water in the composition is at least 30%
w/w, and preferably between 35 to 65% w/w.
TABLE-US-00003 TABLE 3* Ingredient % Concentration (by weight)
Water 63 Titanium dioxide 5 Cyclopentasiloxane 3 C12-15 alkyl
benzoate 3 Octinoxate 3 Methyl methacrylate crosspolymer 3
Neopentyl glycol dicaprate 3 Dipropylene glycol 2 Butylene glycol 2
C14-22 alcohols 2 Oxybenzone 2 Iron oxides 1 Silica 1 Glycerin 1
Stearic acid 1 Benzyl alcohol 0.8 C12-20 alkyl glucoside 0.5
Hydroxyethyl acrylate/sodium 0.4 acryloyldimethyl taurate copolymer
Triethanolamine 0.4 Isohexadecane 0.3 Xanthan gum 0.2 Salicylic
acid 0.1 Disodium EDTA 0.1 Hydrolyzed algin 0.005 Saccharide
isomerate 0.001 Zinc sulfate 0.0005 Opuntia tuna fruit extract
(optional) 0.0005 Excipients** q.s. *Formulation can be prepared by
mixing the ingredients in a beaker under heat 70-75.degree. C.
until homogenous. Subsequently, the formulation can be cooled to
standing room temperature (20-25.degree. C.). Further, and if
desired, additional ingredients can be added, for example, to
modify the rheological properties of the composition. **Excipients
can be added, for example, to modify the rheological properties of
the composition. Alternatively, the amount of water can be varied
so long as the amount of water in the composition is at least 50%
w/w, and preferably between 60 to 90% w/w.
TABLE-US-00004 TABLE 4* Ingredient % Concentration (by weight)
Water 95 Butylene glycol 3 Glycerin 1 Caprylyl glycol 0.4
PPG-5-ceteth-20 0.4 1,2-hexanediol 0.4 Disodium EDTA 0.1 Fragrance
(optional) 0.1 Hydrolyzed algin 0.05 Saccharide isomerate 0.01 Zinc
sulfate 0.005 Opuntia tuna fruit extract (optional) 0.0005
Excipients** q.s. *Formulation can be prepared by mixing the
ingredients in a beaker under heat 70-75.degree. C. until
homogenous. Subsequently, the formulation can be cooled to standing
room temperature (20-25.degree. C.). Further, and if desired,
additional ingredients can be added, for example, to modify the
rheological properties of the composition. **Excipients can be
added, for example, to modify the rheological properties of the
composition. Alternatively, the amount of water can be varied so
long as the amount of water in the composition is at least 80% w/w,
and preferably between 85 to 98% w/w.
TABLE-US-00005 TABLE 5* Ingredient Water Sorbitol Glycerin Disodium
EDTA PEG-32 Chlorphenesin Hydroxyethylcellulose Sodium cocoyl
glycinate Cocamidopropyl betaine Polyglyceryl-4 caprate Hexylene
glycol Salicylic acid PEG-8 Phenoxyethanol Hydrolyzed algin
Saccharide isomerate Zinc sulfate Opuntia tuna fruit extract
(optional) Excipients** *Formulation can be prepared by mixing the
ingredients in a beaker under heat 70-75.degree. C. until
homogenous. Subsequently, the formulation can be cooled to standing
room temperature (20-25.degree. C.). Further, and if desired,
additional ingredients can be added, for example, to modify the
rheological properties of the composition. **Excipients can be
added, for example, to modify the rheological properties of the
composition. Alternatively, the amount of water can be varied so
long as the amount of water in the composition is at least 60% w/w,
and preferably between 60 to 95% w/w.
TABLE-US-00006 TABLE 6* Ingredient Water Sorbitol Glycerin Disodium
EDTA PEG-32 Chlorphenesin TEA-lauryl sulfate Potassium hydroxide
Hexylene glycol Salicylic acid PEG-8 Phenoxyethanol Sodium C14-16
olefin sulfonate Cocamidopropyl hydroxysultaine Hydrolyzed algin
Saccharide isomerate Zinc sulfate Opuntia tuna fruit extract
(optional) Excipients** *Formulation can be prepared by mixing the
ingredients in a beaker under heat 70-75.degree. C. until
homogenous. Subsequently, the formulation can be cooled to standing
room temperature (20-25.degree. C.). Further, and if desired,
additional ingredients can be added, for example, to modify the
rheological properties of the composition. **Excipients can be
added, for example, to modify the rheological properties of the
composition. Alternatively, the amount of water can be varied so
long as the amount of water in the composition is at least 40% w/w,
and preferably between 45 to 95% w/w.
TABLE-US-00007 TABLE 7* Ingredient Water Sorbitol Glycerin Disodium
EDTA PEG-32 Chlorphenesin TEA-lauryl sulfate Potassium hydroxide
Hexylene glycol Salicylic acid PEG-8 Phenoxyethanol Sodium methyl
cocoyl taurate Cocamidopropyl hydroxysultaine Hydrolyzed algin
Saccharide isomerate Zinc sulfate Opuntia tuna fruit extract
(optional) Excipients** *Formulation can be prepared by mixing the
ingredients in a beaker under heat 70-75.degree. C. until
homogenous. Subsequently, the formulation can be cooled to standing
room temperature (20-25.degree. C.). Further, and if desired,
additional ingredients can be added, for example, to modify the
rheological properties of the composition. **Excipients can be
added, for example, to modify the rheological properties of the
composition. Alternatively, the amount of water can be varied so
long as the amount of water in the composition is at least 55% w/w,
and preferably between 60 to 95% w/w.
TABLE-US-00008 TABLE 8* Ingredient Water Sorbitol Glycerin Disodium
EDTA PEG-32 Chlorphenesin TEA-lauryl sulfate Potassium hydroxide
Hexylene glycol Salicylic acid PEG-8 Phenoxyethanol Sodium cocoyl
glycinate Sodium methyl cocoyl taurate Hydrolyzed algin Saccharide
isomerate Zinc sulfate Opuntia tuna fruit extract (optional)
Excipients** *Formulation can be prepared by mixing the ingredients
in a beaker under heat 70-75.degree. C. until homogenous.
Subsequently, the formulation can be cooled to standing room
temperature (20-25.degree. C.). Further, and if desired, additional
ingredients can be added, for example, to modify the rheological
properties of the composition. **Excipients can be added, for
example, to modify the rheological properties of the composition.
Alternatively, the amount of water can be varied so long as the
amount of water in the composition is at least 55% w/w, and
preferably between 60 to 95% w/w.
TABLE-US-00009 TABLE 9* Ingredient % Concentration (by weight)
Water 77 PEG-8 4 TEA-lauryl sulfate 4 Glycerin 3 Sodium methyl
cocoyl taurate 2 Sorbitol 2 Hexylene glycol 1 PEG-32 1
Phenoxyethanol 0.9 Sodium chloride 0.4 Chlorphenesin 0.2 Disodium
EDTA 0.1 Hydroxypropyl cyclodextrin 0.1 Salicylic acid 0.1
Hydrolyzed algin 0.05 Saccharide isomerate 0.01 Zinc sulfate 0.005
Opuntia tuna fruit extract (optional) 0.0005 Excipients** q.s.
*Formulation can be prepared by mixing the ingredients in a beaker
under heat 70-75.degree. C. until homogenous. Subsequently, the
formulation can be cooled to standing room temperature
(20-25.degree. C.). Further, and if desired, additional ingredients
can be added, for example, to modify the rheological properties of
the composition. **Excipients can be added, for example, to modify
the rheological properties of the composition. Alternatively, the
amount of water can be varied so long as the amount of water in the
composition is at least 55% w/w, and preferably between 60 to 95%
w/w.
Example 2
Efficacy of Ingredients
[0097] The efficacy of the ingredients were determined by the
following methods. The following are non-limiting assays that can
be used in the context of the present invention. It should be
recognized that other testing procedures can be used, including,
for example, objective and subjective procedures.
[0098] It was determined that saccharide isomerate increases
keratinocyte production of filaggrin, increases conductance of
artificial skin equivalents, increases keratinocyte production of
occludin, inhibits TNF.alpha. production from keratinocytes, and
has antioxidant capacity. It was also determined that the
combination of hydrolyzed algin and zinc sulfate inhibits
PPAR-.gamma. activity, inhibits MMP1 activity, inhibits MMP9
activity, and inhibits elastase activity. A summary of quantitative
results is found in Table 10 and the method used to determine the
properties of the ingredients are provided below.
TABLE-US-00010 TABLE 10 Ingredient Assay Activity Saccharide
Keratinocyte Production of Filaggrin +28% isomerate Artificial Skin
+79% Keratinocyte Production of Occludin +170% Keratinocyte
Production of TNF.alpha. -88% Antioxidant Capacity +36% Hydrolyzed
PPAR-.gamma. Activity -70% algin and MMP1 Activity -42% Zinc
sulfate MMP9 Activity -37% Elastase Activity -30%
[0099] Production of Filaggrin--
[0100] Saccharide isomerate has been shown to increase keratinocyte
production of filaggrin. Filaggrin is the precursor to Natural
Moisturizing Factor (NMF) in the skin. Increased NMF increases the
moisture content of the skin. Filaggrin production in treated and
non-treated keratinocytes were determined using a bioassay that
analyzes filaggrin concentration in keratinocyte cell lysates. The
bioassay was performed using PROTEINSIMPLE.RTM. Simon.TM. western
blotting protocol. It was determined that saccharide isomerate
increased keratinocyte production of filaggrin by 28%.
[0101] For the samples, normal human epidermal keratinocytes (NHEK)
were grown in EPI-200-Mattek Epilife.RTM. growth media with calcium
from Life Technologies (M-EP-500-CA). NHEK were incubated in growth
medium overnight at 37.degree. C. in 5% CO.sub.2 prior to
treatment. NHEK were then incubated in growth medium with 1% test
compound/extract or no compound/extract for 24 to 36 hours. The
NHEK were then washed, collected, and stored on ice or colder until
lysed on ice using a lysis buffer and sonication. The protein
concentrations of the samples were determined and used to normalize
the samples. The lysates were stored at -80.degree. C. until use in
the bioassay.
[0102] Briefly, the bioassay assay employs a quantitative western
blotting immunoassay technique using an antibody specific for
filaggrin to quantitatively detect filaggrin in the test samples.
Cell samples were lysed and normalized for protein concentration.
Normalized samples and molecular weight standards were then loaded
and ran on a denatured protein separation gel using capillary
electrophoresis. The proteins in the gel were immobilized and
immunoprobed using a primary antibody specific for filaggrin. The
immobilized proteins were then immunoprobed with an enzyme-linked
detection antibody that binds the primary antibody. A
chemiluminescent substrate solution was then added to the
immobilized proteins to allow chemiluminescent development in
proportion to the amount of filaggrin bound in the immobilization.
The chemiluminescent development was stopped at a specific time and
the intensity of the chemiluminescent signal was measured and
compared to positive and negative controls.
[0103] Skin Moisturization/Hydration--
[0104] Saccharide isomerate has been shown to increase a clinical
measurement of skin moisturization using a skin moisture/hydration
assay. This assay determines impedance measurements with the Nova
Dermal Phase Meter. The impedance meter measures changes in skin
moisture content. The outer layer of the skin has distinct
electrical properties. When skin is dry it conducts electricity
very poorly. As it becomes more hydrated increasing conductivity
results. Consequently, changes in skin impedance (related to
conductivity) can be used to assess changes in skin hydration. It
was determined that saccharide isomerate increased conductance of
artificial skin by 79%, indicating increased
moisture/hydration.
[0105] For this assay, treated and non-treated artificial skin
equivalents were used. The Nova Dermal Phase Meter was calibrated
according to instrument instructions for each testing day. A
notation of temperature and relative humidity was made for
comparison purposes. Impedance was evaluated as follows: prior to
measurement, the samples were equilibrate in a room with defined
humidity (e.g., 30-50%) and temperature (e.g., 68-72.degree. C.).
Impedance readings were taken on each sample, recorded, and
averaged. The T5 setting were used on the impedance meter which
averages the impedance values of every five seconds application to
the sample. Changes were reported with statistical variance and
significance.
[0106] Production of Occludin--
[0107] Saccharide isomerate has been shown to increase keratinocyte
production of occludin. Occludin is a protein critical to the
formulation of tight junctions and the skin's moisture barrier
function. Occludin production in treated and non-treated
keratinocytes were determined using a bioassay that analyzes
occludin concentration in keratinocyte cell lysates. The bioassay
was performed using PROTEINSIMPLE.RTM. Simon.TM. western blotting
protocol. It was determined that saccharide isomerate increased
keratinocyte production of occludin by 170%.
[0108] For the samples, adult human epidermal keratinocytes (HEKa)
from Life Technologies (C-005-5C) were grown at 37.degree. C. and
5% CO2 for 24 hours in Epilife growth media with calcium from Life
Technologies (M-EP-500-CA) supplemented with Keratinocyte Growth
Supplement (HKGS) from Life Technologies (S-101-5). HEKa were then
incubated in growth medium with test compound/extract, no
compound/extract for negative control, or with 1 mM CaCl.sub.2 for
positive control for 24 to 48 hours. The HEKa were then washed,
collected, and stored on ice or colder until lysed on ice using a
lysis buffer and sonication. The protein concentrations of the
samples were determined and used to normalize the samples. The
lysates were stored at -80.degree. C. until use in the
bioassay.
[0109] Briefly, the bioassay assay employs a quantitative western
blotting immunoassay technique using an antibody specific for
occludin to quantitatively detect occludin in the test samples.
Cell samples were lysed and normalized for protein concentration.
Normalized samples and molecular weight standards were then loaded
and ran on a denatured protein separation gel using capillary
electrophoresis. The proteins in the gel were immobilized and
immunoprobed using a primary antibody specific for occludin. The
immobilized proteins were then immunoprobed with an enzyme-linked
detection antibody that binds the primary antibody. A
chemiluminescent substrate solution was then added to the
immobilized proteins to allow chemiluminescent development in
proportion to the amount of occludin bound in the immobilization.
The chemiluminescent development was stopped at a specific time and
the intensity of the chemiluminescent signal was measured and
compared to positive and negative controls.
[0110] Inhibition of Tumor Necrosis Factor Alpha
(TNF-.alpha.)--
[0111] Saccharide isomerate has been shown to inhibit TNF-.alpha.
production in keratinocytes. TNF-.alpha. is the prototype ligand of
the TNF superfamily. It is a pleiotropic cytokine that plays a
central role in inflammation. Increase in its expression is
associated with an up regulation in pro-inflammatory activity. The
bioassay used to analyze the effect of saccharide isomerate used a
spectrophotometric measurement that reflects the presence of
TNF-.alpha. and cellular viability. It was determined that
saccharide isomerate inhibits TNF-.alpha. production in
keratinocytes by 88%.
[0112] Subconfluent normal human adult keratinocytes (Cascade
Biologics) cultivated in EpiLife standard growth medium (Cascade
Biologics) at 37.degree. C. in 5% CO2, were treated with phorbol
12-myristate 13-acetate (PMA, 10 ng/ml, Sigma Chemical, #P1585-1MG)
and either saccharide isomerate (treated sample) or no additional
treatment (untreated sample) for 6 hours. PMA causes a dramatic
increase in TNF-.alpha. secretion which peaks at 6 hours after
treatment. Following incubation, cell culture medium was collected
and the amount of TNF-a secretion quantified using a sandwich
enzyme linked immuno-sorbant assay (ELISA) from R&D Systems
(#DTA00C).
[0113] Briefly, the ELISA assay employed the quantitative sandwich
enzyme immunoassay technique whereby a monoclonal antibody specific
for TNF-.alpha. was been pre-coated onto a microplate. Standards
and treated and untreated samples were pipetted into the microplate
wells to allow any TNF-.alpha. present to be bound by the
immobilized antibody. After washing away any unbound substances, an
enzyme-linked polyclonal antibody specific for TNF-.alpha. was
added to the wells. Following a wash to remove any unbound
antibody-enzyme reagent, a substrate solution was added to the
wells to allow color development in proportion to the amount of
TNF-.alpha. bound in the initial step. The color development was
stopped at a specific time and the intensity of the color at 450 nm
was measured using a microplate reader.
[0114] Antioxidant Capacity--
[0115] Saccharide isomerate has been shown to possess antioxidant
capacity. The antioxidant system of living organisms includes
enzymes such as superoxide dismutase, catalase, and glutathione
peroxidase; macromolecules such as albumin, ceruloplasmin, and
ferritin; and an array of small molecules, including ascorbic acid,
.alpha.-tocopherol, .beta.-carotene, reduced glutathione, uric
acid, and bilirubin. The sum of endogenous and food-derived
antioxidants represents the total antioxidant activity of the
extracellular fluid. Cooperation of all the different antioxidants
provides greater protection against attack by reactive oxygen or
nitrogen radicals, than any single compound alone. Thus, the
overall antioxidant capacity may give more relevant biological
information compared to that obtained by the measurement of
individual components, as it accounts for the cumulative effect of
all antioxidants present in plasma and body fluids. It was
determined that saccharide isomerate possesses an antioxidant
capacity of 36% of trolox. Antioxidant capacity indicates a
capability to reduce oxidizing agents (oxidants).
[0116] Antioxidant capacity was determined by an Oxygen Radical
Absorption (or Absorbance) Capacity (ORAC) assay. This assay
quantifies the degree and length of time it takes to inhibit the
action of an oxidizing agent, such as oxygen radicals, that are
known to cause damage to cells (e.g., skin cells). The ORAC value
of control and Saccharide isomerate was determined by the Zen-Bio
ORAC Anti-oxidant Assay kit (#AOX-2). Briefly, this assay measures
the loss of fluorescein fluorescence over time due to the
peroxyl-radical formation by the breakdown of AAPH
(2,2'-axobis-2-methyl propanimidamide, dihydrochloride). Trolox, a
water soluble vitamin E analog, serves as positive control
inhibition fluorescein decay in a dose dependent manner.
[0117] Inhibition of Peroxisome Proliferator-Activated Receptor
Gamma (PPAR-.gamma.)--
[0118] The combination of hydrolyzed algin and zinc sulfate has
been shown to inhibit PPAR-.gamma.. PPAR-.gamma. is a receptor
critical for the production of sebum. The activity of PPAR-.gamma.
in the presence or absence of the combination of hydrolyzed algin
and zinc sulfate was determined using a bioassay that analyzes the
ability of a test compound or composition to inhibit binding of a
ligand. It was determined that the combination of hydrolyzed algin
and zinc sulfate inhibits PPAR-.gamma. activity by 70%.
[0119] Briefly, fluorescent small-molecule pan-PPAR ligand,
FLUORMONE.TM. Pan-PPAR Green, available from Life Technologies
(PV4894), was used to determine if test compounds or compositions
were able to inhibit binding of the ligand to PPAR-.gamma.. The
samples wells included PPAR-.gamma. and fluorescent ligand and
either: test compound or composition (test); a reference inhibitor,
rosiglitazone (positive control); or no test compound (negative
control). The wells were incubated for a set period of time to
allow the ligand opportunity to bind the PPAR-.gamma.. The
fluorescence polarization of each sample well was measured and
compared to the negative control well to determine the percentage
of inhibition by the test compound or composition.
[0120] Inhibition of Matrix Metalloproteinase 1 Enzyme (MMP1)--
[0121] The combination of hydrolyzed algin and zinc sulfate has
been shown to inhibit MMP1. MMPs are extracellular proteases that
play a role in many normal and disease states by virtue of their
broad substrate specificity. MMP1 substrates include collagen IV.
The activity of MMP1 in the presence or absence of the combination
of hydrolyzed algin and zinc sulfate was determined using the
Molecular Probes Enz/Chek Gelatinase/Collagenase Assay kit
(#E12055). It was determined that the combination of hydrolyzed
algin and zinc sulfate inhibits MMP1 activity by 42%.
[0122] Briefly, this kit utilizes a fluorogenic gelatin substrate
to detect MMP1 protease activity in vitro. Upon proteolytic
cleavage of the fluorogenic gelatin substrate, bright green
fluorescence was revealed and was monitored using a fluorescent
microplate reader to measure enzymatic activity. Test materials
were incubated in the presence or absence of the purified enzyme
and substrate to determine their protease inhibitor capacity.
[0123] Inhibition of Matrix Metalloproteinase 9 Enzyme (MMP9)--
[0124] The combination of hydrolyzed algin and zinc sulfate has
been shown to inhibit MMP9. MMPs are extracellular proteases that
play a role in many normal and disease states by virtue of their
broad substrate specificity. MMP9 substrates include collagen VII,
fibronectins and laminin. The activity of MMP9 in the presence or
absence of the combination of hydrolyzed algin and zinc sulfate was
determined using the Colorimetric Drug Discovery kit from BioMol
International for MMP9 (AK-410). It was determined that the
combination of hydrolyzed algin and zinc sulfate inhibits MMP9
activity by 37%.
[0125] This assay is designed to measure protease activity of MMPs
using a thiopeptide as a chromogenic substrate
(Ac-PLG-[2-mercapto-4-methyl-pentanoyl]-LG-OC2H5)5,6. The MMP9
cleavage site peptide bond was replaced by a thioester bond in the
thiopeptide. Hydrolysis of this bond by MMP9 produced a sulfhydryl
group, which reacts with DTNB [5,5'-dithiobis(2-nitrobenzoic acid),
Ellman's reagent] which formed 2-nitro-5-thiobenzoic acid, which
was detected by its absorbance at 412 nm (.epsilon.=13,600 M-1 cm-1
at pH 6.0 and above 7).
[0126] Inhibition of Elastase Activity--
[0127] The combination of hydrolyzed algin and zinc sulfate has
been shown to inhibit elastase activity. Elastase is an enzyme that
degrades elastin. The combination's inhibition of elastase activity
was determined using an EnzChek.RTM. Elastase Assay (Kit# E-12056)
from Molecular Probes (Eugene, Oreg. USA). This kit was used as an
in vitro enzyme inhibition assay for measuring inhibition of
elastase activity. It was determined that the combination of
hydrolyzed algin and zinc sulfate inhibits elastase activity by
30%.
[0128] Briefly, the EnzChek kit contains soluble bovine neck
ligament elastin that is labeled with dye such that the conjugate's
fluorescence is quenched. The non-fluorescent bovine neck ligament
elastin substrate is digested by elastase or other proteases to
yield highly fluorescent fragments. The resulting increase in
fluorescence is monitored with a fluorescence microplate reader.
Digestion products from the elastin substrate have absorption
maxima at .about.505 nm and fluorescence emission maxima at
.about.515 nm. No treatment or the combination of hydrolyzed algin
and zinc sulfate were added into the digestion reaction to
determine inhibition of elastase. As a positive control,
N-methoxysuccinyl-Ala-Ala-Pro-Val-chloromethyl ketone was used as
selective, collective inhibitor of elastase activity.
Example 3
Additional Assays
[0129] Assays that can be used to determine the efficacy of any one
of the ingredients or any combination of ingredients or
compositions having said combination of ingredients disclosed
throughout the specification and claims can be determined by
methods known to those of ordinary skill in the art. The following
are non-limiting assays that can be used in the context of the
present invention. It should be recognized that other testing
procedures can be used, including, for example, objective and
subjective procedures.
[0130] B16 Pigmentation Assay:
[0131] Melanogenesis is the process by which melanocytes produce
melanin, a naturally produced pigment that imparts color to skin,
hair, and eyes. Inhibiting melanogenesis is beneficial to prevent
skin darkening and lighten dark spots associated with aging. This
bioassay utilizes B16-F1 melanocytes (ATCC), an immortalized mouse
melanoma cell line, to analyze the effect of compounds on
melanogenesis. The endpoint of this assay is a spectrophotometric
measurement of melanin production and cellular viability. B16-F1
melanocytes, can be cultivated in standard DMEM growth medium with
10% fetal bovine serum (Mediatech) at 37.degree. C. in 10% CO.sub.2
and then treated with any one of the active ingredients,
combination of ingredients, or compositions having said
combinations disclosed in the specification for 6 days. Following
incubation, melanin secretion is measured by absorbance at 405 nm
and cellular viability is quantified.
[0132] Collagen Stimulation Assay:
[0133] Collagen is an extracellular matrix protein critical for
skin structure. Increased synthesis of collagen helps improve skin
firmness and elasticity. This bioassay can be used to examine the
effect of any one of the active ingredients, combination of
ingredients, or compositions having said combinations disclosed in
the specification on the production of procollagen peptide (a
precursor to collagen) by human epidermal fibroblasts. The endpoint
of this assay is a spectrophotometric measurement that reflects the
presence of procollagen peptide and cellular viability. The assay
employs the quantitative sandwich enzyme immunoassay technique
whereby a monoclonal antibody specific for procollagen peptide has
been pre-coated onto a microplate. Standards and samples can be
pipetted into the wells and any procollagen peptide present is
bound by the immobilized antibody. After washing away any unbound
substances, an enzyme-linked polyclonal antibody specific for
procollagen peptide can be added to the wells. Following a wash to
remove any unbound antibody-enzyme reagent, a substrate solution
can be added to the wells and color develops in proportion to the
amount of procollagen peptide bound in the initial step using a
microplate reader for detection at 450 nm. The color development
can be stopped and the intensity of the color can be measured.
Subconfluent normal human adult epidermal fibroblasts (Cascade
Biologics) cultivated in standard DMEM growth medium with 10% fetal
bovine serum (Mediatech) at 37.degree. C. in 10% CO.sub.2, can be
treated with each of the combination of ingredients or compositions
having said combinations disclosed in the specification for 3 days.
Following incubation, cell culture medium can be collected and the
amount of procollagen peptide secretion quantified using a sandwich
enzyme linked immuno-sorbant assay (ELISA) from Takara
(#MK101).
[0134] Elastin Stimulation Assay:
[0135] Elastin is a connective tissue protein that helps skin
resume shape after stretching or contracting. Elastin is also an
important load-bearing protein used in places where mechanical
energy is required to be stored. Elastin is made by linking many
soluble tropoelastin protein molecules, in a reaction catalyzed by
lysyl oxidase. Elastin secretion and elastin fibers can be
monitored in cultured human fibroblasts by staining of cultured
human fibroblasts using immunofluorescent antibodies directed
against elastin.
[0136] Laminin Stimulation Assay:
[0137] Laminin and fibronectin are major proteins in the
dermal-epidermal junction (DEJ) (also referred to as the basement
membrane). The DEJ is located between the dermis and the epidermis
interlocks forming fingerlike projections called rete ridges. The
cells of the epidermis receive their nutrients from the blood
vessels in the dermis. The rete ridges increase the surface area of
the epidermis that is exposed to these blood vessels and the needed
nutrients. The DEJ provides adhesion of the two tissue compartments
and governs the structural integrity of the skin. Laminin and
fibronectin are two structural glycoproteins located in the DEJ.
Considered the glue that holds the cells together, laminin and
fibronectin are secreted by dermal fibroblasts to help facilitate
intra- and inter-cellular adhesion of the epidermal calls to the
DEJ. Laminin secretion can be monitored by quantifying laminin in
cell supernatants of cultured human fibroblasts treated for 3 days
with culture medium with or without 1.0% final concentration of the
test ingredient(s). Following incubation, laminin content can be
measured using immunofluorescent antibodies directed against
laminin in an enzyme linked immuno-sorbant assay (ELISA).
Measurements are normalized for cellular metabolic activity, as
determined by bioconversion of
3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-
-2H-tetrazolium (MTS).
[0138] Antioxidant (AO) Assay:
[0139] An in vitro bioassay that measures the total anti-oxidant
capacity of any one of the ingredients, combination of ingredients,
or compositions having said combinations disclosed in the
specification. The assay relies on the ability of antioxidants in
the sample to inhibit the oxidation of ABTS.RTM.
(2,2'-azino-di-[3-ethylbenzthiazoline sulphonate]) to ABTS.RTM.+ by
metmyoglobin. The antioxidant system of living organisms includes
enzymes such as superoxide dismutase, catalase, and glutathione
peroxidase; macromolecules such as albumin, ceruloplasmin, and
ferritin; and an array of small molecules, including ascorbic acid,
.alpha.-tocopherol, .beta.-carotene, reduced glutathione, uric
acid, and bilirubin. The sum of endogenous and food-derived
antioxidants represents the total antioxidant activity of the
extracellular fluid. Cooperation of all the different antioxidants
provides greater protection against attack by reactive oxygen or
nitrogen radicals, than any single compound alone. Thus, the
overall antioxidant capacity may give more relevant biological
information compared to that obtained by the measurement of
individual components, as it considers the cumulative effect of all
antioxidants present in plasma and body fluids. The capacity of the
antioxidants in the sample to prevent ABTS oxidation is compared
with that of Trolox, a water-soluble tocopherol analogue, and is
quantified as molar Trolox equivalents. Anti-Oxidant capacity kit
#709001 from Cayman Chemical (Ann Arbor, Mich. USA) can be used as
an in vitro bioassay to measure the total anti-oxidant capacity of
each of any one of the active ingredients, combination of
ingredients, or compositions having said combinations disclosed in
the specification. The protocol can be followed according to
manufacturer recommendations. The assay relied on antioxidants in
the sample to inhibit the oxidation of ABTS.RTM.
(2,2'-azino-di-[3-ethylbenzthiazoline sulphonate]) to ABTS.RTM.+ by
metmyoglobin. The capacity of the antioxidants in the sample to
prevent ABTS oxidation can be compared with that Trolox, a
water-soluble tocopherol analogue, and can be quantified as a molar
Trolox equivalent.
[0140] Mushroom Tyrosinase Activity Assay:
[0141] In mammalian cells, tyrosinase catalyzes two steps in the
multi-step biosynthesis of melanin pigments from tyrosine (and from
the polymerization of dopachrome). Tyrosinase is localized in
melanocytes and produces melanin (aromatic quinone compounds) that
imparts color to skin, hair, and eyes. Purified mushroom tyrosinase
(Sigma) can be incubated with its substrate L-Dopa (Fisher) in the
presence or absence of each of the active ingredients, any one of
the combination of ingredients, or compositions having said
combinations disclosed in the specification. Pigment formation can
be evaluated by colorimetric plate reading at 490 nm. The percent
inhibition of mushroom tyrosinase activity can be calculated
compared to non-treated controls to determine the ability of test
ingredients or combinations thereof to inhibit the activity of
purified enzyme. Test extract inhibition was compared with that of
kojic acid (Sigma).
[0142] Matrix Metalloproteinase 3 and 9 Enzyme Activity (MMP3;
MMP9) Assay:
[0143] An in vitro matrix metalloprotease (MMP) inhibition assay.
MMPs are extracellular proteases that play a role in many normal
and disease states by virtue of their broad substrate specificity.
MMP3 substrates include collagens, fibronectins, and laminin; while
MMP9 substrates include collagen VII, fibronectins and laminin.
Using Colorimetric Drug Discovery kits from BioMol International
for MMP3 (AK-400) and MMP-9 (AK-410), this assay is designed to
measure protease activity of MMPs using a thiopeptide as a
chromogenic substrate
(Ac-PLG-[2-mercapto-4-methyl-pentanoyl]-LG-OC2H5)5,6. The MMP
cleavage site peptide bond is replaced by a thioester bond in the
thiopeptide. Hydrolysis of this bond by an MMP produces a
sulfhydryl group, which reacts with DTNB
[5,5'-dithiobis(2-nitrobenzoic acid), Ellman's reagent] to form
2-nitro-5-thiobenzoic acid, which can be detected by its absorbance
at 412 nm (.epsilon.=13,600 M-1 cm-1 at pH 6.0 and above 7). The
active ingredients, any one of the combination of ingredients, or
compositions having said combinations disclosed in the
specification can be assayed.
[0144] Cyclooxygenase (COX) Assay:
[0145] An in vitro cyclooxygenase-1 and -2 (COX-1, -2) inhibition
assay. COX is a bifunctional enzyme exhibiting both cyclooxygenase
and peroxidase activities. The cyclooxygenase activity converts
arachidonic acid to a hydroperoxy endoperoxide (Prostaglandin G2;
PGG2) and the peroxidase component reduces the endoperoxide
(Prostaglandin H2; PGH2) to the corresponding alcohol, the
precursor of prostaglandins, thromboxanes, and prostacyclins. This
COX Inhibitor screening assay measures the peroxidase component of
cyclooxygenases. The peroxidase activity is assayed
colorimetrically by monitoring the appearance of oxidized
N,N,N',N'-tetramethyl-p-phenylenediamine (TMPD). This inhibitor
screening assay includes both COX-1 and COX-2 enzymes in order to
screen isozyme-specific inhibitors. The Colormetric COX (ovine)
Inhibitor screening assay (#760111, Cayman Chemical) can be used to
analyze the effects of each of the active ingredients, any one of
the combination of ingredients, or compositions having said
combinations disclosed in the specification on the activity of
purified cyclooxygnase enzyme (COX-1 or COX-2). According to
manufacturer instructions, purified enzyme, heme and test extracts
can be mixed in assay buffer and incubated with shaking for 15 min
at room temperature. Following incubation, arachidonic acid and
colorimetric substrate can be added to initiate the reaction. Color
progression can be evaluated by colorimetric plate reading at 590
nm. The percent inhibition of COX-1 or COX-2 activity can be
calculated compared to non-treated controls to determine the
ability of test extracts to inhibit the activity of purified
enzyme.
[0146] Lipoxygenase (LO) Assay:
[0147] An in vitro lipoxygenase (LO) inhibition assay. LOs are
non-heme iron-containing dioxygenases that catalyze the addition of
molecular oxygen to fatty acids. Linoleate and arachidonate are the
main substrates for LOs in plants and animals. Arachadonic acid may
then be converted to hydroxyeicosotrienenoic (HETE) acid
derivatives, that are subsequently converted to leukotrienes,
potent inflammatory mediators. This assay provides an accurate and
convenient method for screening lipoxygenase inhibitors by
measuring the hydroperoxides generated from the incubation of a
lipoxygenase (5-, 12-, or 15-LO) with arachidonic acid. The
Colorimetric LO Inhibitor screening kit (#760700, Cayman Chemical)
can be used to determine the ability of each of the active
ingredients, any one of the combination of ingredients, or
compositions having said combinations disclosed in the
specification to inhibit enzyme activity. Purified 15-lipoxygenase
and test ingredients can be mixed in assay buffer and incubated
with shaking for 10 min at room temperature. Following incubation,
arachidonic acid can be added to initiate the reaction and the
mixtures can be incubated for an additional 10 min at room
temperature. Colorimetric substrate can be added to terminate
catalysis and color progression can be evaluated by fluorescence
plate reading at 490 nm. The percent inhibition of lipoxyganse
activity can be calculated compared to non-treated controls to
determine the ability of each of the active ingredients, any one of
the combination of ingredients, or compositions having said
combinations disclosed in the specification to inhibit the activity
of purified enzyme.
[0148] Oil Control Assay:
[0149] An assay to measure reduction of sebum secretion from
sebaceous glands and/or reduction of sebum production from
sebaceous glands can be assayed by using standard techniques known
to those having ordinary skill in the art. In some aspects, the
forehead can be used. Each of the active ingredients, any one of
the combination of ingredients, or compositions having said
combinations disclosed in the specification can be applied to one
portion of the forehead once or twice daily for a set period of
days (e.g., 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, or more
days), while another portion of the forehead is not treated with
the composition. After the set period of days expires, then sebum
secretion can be assayed by application of fine blotting paper to
the treated and untreated forehead skin. This is done by first
removing any sebum from the treated and untreated areas with moist
and dry cloths. Blotting paper can then be applied to the treated
and untreated areas of the forehead, and an elastic band can be
placed around the forehead to gently press the blotting paper onto
the skin. After 2 hours the blotting papers can be removed, allowed
to dry and then transilluminated. Darker blotting paper correlates
with more sebum secretion (or lighter blotting paper correlates
with reduced sebum secretion.
[0150] Erythema Assay:
[0151] An assay to measure the reduction of skin redness can be
evaluated using a Minolta Chromometer. Skin erythema may be induced
by applying a 0.2% solution of sodium dodecyl sulfate on the
forearm of a subject. The area is protected by an occlusive patch
for 24 hrs. After 24 hrs, the patch is removed and the
irritation-induced redness can be assessed using the a* values of
the Minolta Chroma Meter. The a* value measures changes in skin
color in the red region. Immediately after reading, the area is
treated with the active ingredients, any one of the combination of
ingredients, or compositions having said combinations disclosed in
the specification. Repeat measurements can be taken at regular
intervals to determine the formula's ability to reduce redness and
irritation.
[0152] Skin Clarity and Reduction in Freckles and Age Spots
Assay:
[0153] Skin clarity and the reduction in freckles and age spots can
be evaluated using a Minolta Chromometer. Changes in skin color can
be assessed to determine irritation potential due to product
treatment using the a* values of the Minolta Chroma Meter. The a*
value measures changes in skin color in the red region. This is
used to determine whether each of the active ingredients, any one
of the combination of ingredients, or compositions having said
combinations disclosed in the specification is inducing irritation.
The measurements can be made on each side of the face and averaged,
as left and right facial values. Skin clarity can also be measured
using the Minolta Meter. The measurement is a combination of the
a*, b, and L values of the Minolta Meter and is related to skin
brightness, and correlates well with skin smoothness and hydration.
Skin reading is taken as above. In one non-limiting aspect, skin
clarity can be described as L/C where C is chroma and is defined as
(a.sup.2+b.sup.2).sup.1/2.
[0154] Skin Dryness, Surface Fine Lines, Skin Smoothness, and Skin
Tone Assay:
[0155] Skin dryness, surface fine lines, skin smoothness, and skin
tone can be evaluated with clinical grading techniques. For
example, clinical grading of skin dryness can be determined by a
five point standard Kligman Scale: (0) skin is soft and moist; (1)
skin appears normal with no visible dryness; (2) skin feels
slightly dry to the touch with no visible flaking; (3) skin feels
dry, tough, and has a whitish appearance with some scaling; and (4)
skin feels very dry, rough, and has a whitish appearance with
scaling. Evaluations can be made independently by two clinicians
and averaged.
[0156] Clinical Grading of Skin Tone Assay:
[0157] Clinical grading of skin tone can be performed via a ten
point analog numerical scale: (10) even skin of uniform, pinkish
brown color. No dark, erythremic, or scaly patches upon examination
with a hand held magnifying lens. Microtexture of the skin very
uniform upon touch; (7) even skin tone observed without
magnification. No scaly areas, but slight discolorations either due
to pigmentation or erythema. No discolorations more than 1 cm in
diameter; (4) both skin discoloration and uneven texture easily
noticeable. Slight scaliness. Skin rough to the touch in some
areas; and (1) uneven skin coloration and texture. Numerous areas
of scaliness and discoloration, either hypopigmented, erythremic or
dark spots. Large areas of uneven color more than 1 cm in diameter.
Evaluations were made independently by two clinicians and
averaged.
[0158] Clinical Grading of Skin Smoothness Assay:
[0159] Clinical grading of skin smoothness can be analyzed via a
ten point analog numerical scale: (10) smooth, skin is moist and
glistening, no resistance upon dragging finger across surface; (7)
somewhat smooth, slight resistance; (4) rough, visibly altered,
friction upon rubbing; and (1) rough, flaky, uneven surface.
Evaluations were made independently by two clinicians and
averaged.
[0160] Skin Smoothness and Wrinkle Reduction Assay With Methods
Disclosed in Packman et al. (1978):
[0161] Skin smoothness and wrinkle reduction can also be assessed
visually by using the methods disclosed in Packman et al. (1978).
For example, at each subject visit, the depth, shallowness and the
total number of superficial facial lines (SFLs) of each subject can
be carefully scored and recorded. A numerical score was obtained by
multiplying a number factor times a depth/width/length factor.
Scores are obtained for the eye area and mouth area (left and right
sides) and added together as the total wrinkle score.
[0162] Skin Firmness Assay with a Hargens Ballistometer:
[0163] Skin firmness can be measured using a Hargens ballistometer,
a device that evaluates the elasticity and firmness of the skin by
dropping a small body onto the skin and recording its first two
rebound peaks. The ballistometry is a small lightweight probe with
a relatively blunt tip (4 square mm-contact area) was used. The
probe penetrates slightly into the skin and results in measurements
that are dependent upon the properties of the outer layers of the
skin, including the stratum corneum and outer epidermis and some of
the dermal layers.
[0164] Skin Softness/Suppleness Assay with a Gas Bearing
Electrodynamometer:
[0165] Skin softness/suppleness can be evaluated using the Gas
Bearing Electrodynamometer, an instrument that measures the
stress/strain properties of the skin. The viscoelastic properties
of skin correlate with skin moisturization. Measurements can be
obtained on the predetermined site on the cheek area by attaching
the probe to the skin surface with double-stick tape. A force of
approximately 3.5 gm can be applied parallel to the skin surface
and the skin displacement is accurately measured. Skin suppleness
can then be calculated and is expressed as DSR (Dynamic Spring Rate
in gm/mm).
[0166] Appearance of Lines and Wrinkles Assay with Replicas:
[0167] The appearance of lines and wrinkles on the skin can be
evaluated using replicas, which is the impression of the skin's
surface. Silicone rubber like material can be used. The replica can
be analyzed by image analysis. Changes in the visibility of lines
and wrinkles can be objectively quantified via the taking of
silicon replicas form the subjects' face and analyzing the replicas
image using a computer image analysis system. Replicas can be taken
from the eye area and the neck area, and photographed with a
digital camera using a low angle incidence lighting. The digital
images can be analyzed with an image processing program and are of
the replicas covered by wrinkles or fine lines was determined.
[0168] Surface Contour of the Skin Assay with a Profilometer/Stylus
Method:
[0169] The surface contour of the skin can be measured by using the
profilometer/Stylus method. This includes either shining a light or
dragging a stylus across the replica surface. The vertical
displacement of the stylus can be fed into a computer via a
distance transducer, and after scanning a fixed length of replica a
cross-sectional analysis of skin profile can be generated as a
two-dimensional curve. This scan can be repeated any number of
times along a fix axis to generate a simulated 3-D picture of the
skin. Ten random sections of the replicas using the stylus
technique can be obtained and combined to generate average values.
The values of interest include Ra which is the arithmetic mean of
all roughness (height) values computed by integrating the profile
height relative to the mean profile height. Rt which is the maximum
vertical distance between the highest peak and lowest trough, and
Rz which is the mean peak amplitude minus the mean peak height.
Values are given as a calibrated value in mm. Equipment should be
standardized prior to each use by scanning metal standards of know
values. Ra Value can be computed by the following equation:
R.sub.a=Standardize roughness; l.sub.m=the traverse (scan) length;
and y=the absolute value of the location of the profile relative to
the mean profile height (x-axis).
[0170] MELANODERM.TM. Assay:
[0171] In other non-limiting aspects, the efficacy of each of the
active ingredients, any one of the combination of ingredients, or
compositions having said combinations disclosed in the
specification can be evaluated by using a skin analog, such as, for
example, MELANODERM.TM.. Melanocytes, one of the cells in the skin
analog, stain positively when exposed to L-dihydroxyphenyl alanine
(L-DOPA), a precursor of melanin. The skin analog, MELANODERM.TM.,
can be treated with a variety of bases containing each of the
active ingredients, any one of the combination of ingredients, or
compositions having said combinations disclosed in the
specification or with the base alone as a control. Alternatively,
an untreated sample of the skin analog can be used as a
control.
[0172] Keratinocyte Monolayer Permeability--
[0173] Changes in the permeability of a keratinocyte monolayer due
to each of the active ingredients, any one of the combination of
ingredients, or compositions having said combinations disclosed in
the specification can be measured. Keratinocyte monolayer
permeability is a measure of skin barrier integrity. Keratinocyte
monolayer permeability in treated and non-treated keratinocytes can
be determined using, as a non-limiting example, the In Vitro
Vascular Permeability assay by Millipore (ECM642). This assay
analyzes endothelial cell adsorption, transport, and permeability.
Briefly, adult human epidermal keratinocytes from Life Technologies
(C-005-5C) can be seeded onto a porous collagen-coated membrane
within a collection well. The keratinocytes are then incubated for
24 hours at 37.degree. C. and 5% CO.sub.2 in Epilife growth media
with calcium from Life Technologies (M-EP-500-CA) supplemented with
Keratinocyte Growth Supplement (HKGS) from Life Technologies
(S-101-5). This incubation time allows the cells to form a
monolayer and occlude the membrane pores. The media is then
replaced with fresh media with (test sample) or without
(non-treated control) test compounds/extracts and the keratinocytes
are incubated for an additional 48 hours at 37.degree. C. and 5%
CO.sub.2. To determine permeability of the keratinocyte monolayer
after incubation with/without the test compound/extract, the media
is replaced with fresh media containing a high molecular weight
Fluorescein isothiocyanate (FITC)-Dextran and the keratinocytes are
incubated for 4 hours at 37.degree. C. and 5% CO.sub.2. During the
4 hours incubation, FITC can pass through the keratinocytes
monolayer and porous membrane into the collection well at a rate
proportional to the monolayer's permeability. After the 4 hour
incubation, cell viability and the content of FITC in the
collection wells can be determined. For the FITC content, the media
in the collection well is collected and fluorescence of the media
determined at 480 nm (Em) when excited at 520 nm. Percent
permeability and percent change in comparison to the non-treated
controls can be determined by the following equations: Percent
Permeability=((Mean Ex/Em of test sample)/Mean Ex/Em untreated
control)*100; Percent Change=Percent Permeability of test
sample-Percent Permeability of untreated control.
[0174] Production of Hyaluronic Acid--
[0175] Changes in the production of hyaluronic acid in human dermal
fibroblasts due to each of the active ingredients, any one of the
combination of ingredients, or compositions having said
combinations disclosed in the specification can be measured. HA is
a polysaccharide involved in stabilization of the structure of the
matrix and is involved in providing turgor pressure to tissue and
cells. As one non-limiting example, HA production in treated and
non-treated adult human dermal fibroblasts (HDFa) cells can be
determined using the Hyaluronan DuoSet ELISA kit from R&D
Systems (DY3614). In this assay, for production of samples,
subconfluent HDFa cells from Cascade Biologics (C-13-5C) are
incubated at 37.degree. C. and 10% CO.sub.2 in starvation medium
(0.15% fetal bovine serum and 1% Penicillin Streptomycin solution
in Dulbecco's Modified Eagle Medium) for 72 hours prior to
treatment. The cells are then incubated with fresh starvation
medium with either test compound, positive control (phorbol
12-myristate 13-acetate from Sigma-Aldrich (P1585) and platelet
derived growth factor from Sigma-Aldrich (P3201)), or no additive
for 24 hours. Media is then collected and frozen at -80.degree. C.
until use in the ELISA assay.
[0176] Briefly, the ELISA assay employs a quantitative sandwich
enzyme immunoassay technique whereby a capture antibody specific
for HA can be pre-coated onto a microplate. Standards and media
from treated and untreated cells are pipetted into the microplate
wells to enable any HA present to be bound by the immobilized
antibody. After washing away any unbound substances, an
enzyme-linked detection antibody specific for HA is added to the
wells. Following a wash to remove any unbound antibody-enzyme
reagent, a substrate solution is added to the wells to allow color
development in proportion to the amount of HA bound in the initial
step. The color development is stopped at a specific time and the
intensity of the color at 450 nm can be measured using a microplate
reader.
[0177] Inhibition of Hyaluronidase Activity--
[0178] Changes in the activity of hyaluronidase due to each of the
active ingredients, any one of the combination of ingredients, or
compositions having said combinations disclosed in the
specification can be measured. Hyaluronidase is an enzyme that
degrades HA. HA is a polysaccharide involved in stabilization of
the structure of the matrix and is involved in providing turgor
pressure to tissue and cells. As one non-limiting example,
hyaluronidase activity can be determined using an in vitro protocol
modified from Sigma-Aldrich protocol # EC 3.2.1.35. Briefly,
hyaluronidase type 1-S from Sigma-Aldrich (H3506) is added to
microplate reaction wells containing test compound or controls.
Tannic acid can be used as a positive control inhibitor, no test
compound can be added for the control enzyme, and wells with test
compound or positive control but without hyaluronidase can be used
as a background negative control. The wells are incubated at
37.degree. C. for 10 minutes before addition of substrate (HA).
Substrate is added and the reactions incubated at 37.degree. C. for
45 minutes. A portion of each reaction solution is then transferred
to and gently mixed in a solution of sodium acetate and acetic acid
pH 3.75 to stop that portion of the reaction (stopped wells). The
stopped wells and the reaction wells should both contain the same
volume of solution after addition of the portion of the reaction
solution to the stopped wells. Both the reaction wells and the
stopped wells are incubated for 10 minutes at room temperature.
Absorbance at 600 nm is then measured for both the reaction wells
and the stopped wells. Inhibition can be calculated using the
following formulas: Inhibitor (or control) activity=(Inhibitor
stopped wells absorbance at 600 nm-inhibitor reaction wells
absorbance at 600 nm); Initial activity=control enzyme absorbance
at 600 nm; Percent Inhibition=[(Initial activity/Inhibitor
Activity)*100]-100.
[0179] All of the compositions and/or methods disclosed and claimed
herein can be made and executed without undue experimentation in
light of the present disclosure. While the compositions and methods
of this invention have been described in terms of preferred
embodiments, it will be apparent to those of skill in the art that
variations may be applied to the compositions and/or methods and in
the steps or in the sequence of steps of the method described
herein without departing from the concept, spirit and scope of the
invention. More specifically, it will be apparent that certain
agents which are both chemically and physiologically related may be
substituted for the agents described herein while the same or
similar results would be achieved. All such similar substitutes and
modifications apparent to those skilled in the art are deemed to be
within the spirit, scope and concept of the invention as defined by
the appended claims.
REFERENCES
[0180] The following references, to the extent that they provide
exemplary procedural or other details supplementary to those set
forth herein, are specifically incorporated herein by reference.
[0181] Cosmetic Ingredient Dictionary, Third Edition, CTFA, 1982
[0182] International Cosmetic Ingredient Dictionary, Fourth
edition, CTFA, 1991 [0183] International Cosmetic Ingredient
Dictionary and Handbook, Tenth Edition, CTFA, 2004 [0184]
International Cosmetic Ingredient Dictionary and Handbook, Twelfth
Edition, CTFA, 2008
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